Relevant bibliographies by topics / Antitumor

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  1. Journal articles
  2. Dissertations / Theses
  3. Books
  4. Book chapters
  5. Conference papers
  6. Reports

Academic literature on the topic 'Antitumor'

Author: Grafiati
Published: 4 June 2021
Last updated: 6 September 2023

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Journal articles on the topic "Antitumor"

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Shtemenko, A. V., and N. I. Shtemenko. "Rhenium–platinum antitumor systems." Ukrainian Biochemical Journal 89, no. 2 (April 24, 2017): 5–30. http://dx.doi.org/10.15407/ubj89.02.005.

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Didenko, G. V. "ANTITUMOR AND ANTIMETASTATIC EFFICIENCY OF ANTITUMOR VACCINE AND AMIXIN COMBINED ACTION IN MICE WITH LEWIS LUNG CARCINOMA." Biotechnologia Acta 9, no. 3 (June 2016): 76–83. http://dx.doi.org/10.15407/biotech9.03.076.

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Asche, Christian, and Martine Demeunynck. "Antitumor Carbazoles." Anti-Cancer Agents in Medicinal Chemistry 7, no. 2 (March 1, 2007): 247–67. http://dx.doi.org/10.2174/187152007780058678.

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Scuderi, N., and M. G. Onesti. "Antitumor Agents." Annals of Plastic Surgery 32, no. 1 (January 1994): 39–44. http://dx.doi.org/10.1097/00000637-199401000-00008.

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NISHIKAWA, KIYOHIRO, CHIEKO SHIBASAKI, KATSUTOSHI TAKAHASHI, TERUYA NAKAMURA, TOMIO TAKEUCHI, and HAMAO UMEZAWA. "Antitumor activity of spergualin, a novel antitumor antibiotic." Journal of Antibiotics 39, no. 10 (1986): 1461–66. http://dx.doi.org/10.7164/antibiotics.39.1461.

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Akima, Kazuo, Hisashi Ito, Yuhei Iwata, Kayoko Matsuo, Nobutoshi Watari, Mitsuo Yanagi, Hiroo Hagi, et al. "Evaluation of antitumor activities of hyaluronate binding antitumor drugs: synthesis, characterization and antitumor activity." Journal of Drug Targeting 4, no. 1 (January 1996): 1–8. http://dx.doi.org/10.3109/10611869609046255.

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Maksimov, Maksim Leonidovich, and Malika Anarbekovna Ismailova. "Adverse reactions during chemotherapy: skin toxicity." Vrač skoroj pomoŝi (Emergency Doctor), no. 9 (September 1, 2020): 28–64. http://dx.doi.org/10.33920/med-02-2009-01.

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Chemotherapy of oncological diseases is associated with high toxicity. The occurrence of various toxic reactions during the use of antitumor drugs is explained by the fact that most antitumor medicines are not strictly specific, therefore, their effect can extend not only to tumor cells, but also to normal cells, especially to tissues with rapid proliferation. All antitumour agents have skin toxicity in one form or another. However, for some chemotherapeutic agents, skin toxicity is a kind of «reflection» of certain mechanisms of drugs action, and, in most cases, the severity of dermatological reactions correlates with the effectiveness of chemotherapy. Dermatological toxicity deserves special attention, as it affects the quality of life of cancer patients and, in some cases, may require a dose reduction or even cancellation of chemotherapy. This article presents current data on the mechanisms of development of skin toxicity of routine chemotherapeutic agents, growth factor inhibitors and some antitumor antibiotics, its correction and prevention opportunities.
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Torres, Nicolas, María Victoria Regge, Florencia Secchiari, Adrián David Friedrich, Raúl Germán Spallanzani, Ximena Lucía Raffo Iraolagoitia, Sol Yanel Núñez, et al. "Restoration of antitumor immunity through anti-MICA antibodies elicited with a chimeric protein." Journal for ImmunoTherapy of Cancer 8, no. 1 (June 2020): e000233. http://dx.doi.org/10.1136/jitc-2019-000233.

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BackgroundNatural killer and cytotoxic CD8+T cells are major players during antitumor immunity. They express NKG2D, an activating receptor that promotes tumor elimination through recognition of the MHC class I chain-related proteins A and B (MICA and MICB). Both molecules are overexpressed on a great variety of tumors from different tissues, making them attractive targets for immunotherapy. However, tumors shed MICA and MICB, and the soluble forms of both (sMICA and sMICB) mediate tumor-immune escape. Some reports indicate that anti-MICA antibodies (Ab) can promote the restoration of antitumor immunity through the induction of direct antitumor effects (antibody-dependent cell-mediated cytotoxicity, ADCC) and scavenging of sMICA. Therefore, we reasoned that an active induction of anti-MICA Ab with an immunogenic protein might represent a novel therapeutic and prophylactic alternative to restore antitumor immunity.MethodsWe generated a highly immunogenic chimeric protein (BLS-MICA) consisting of human MICA fused to the lumazine synthase fromBrucellaspp (BLS) and used it to generate anti-MICA polyclonal Ab (pAb) and to investigate if these anti-MICA Ab can reinstate antitumor immunity in mice using two different mouse tumors engineered to express MICA. We also explored the underlying mechanisms of this expected therapeutic effect.ResultsImmunization with BLS-MICA and administration of anti-MICA pAb elicited by BLS-MICA significantly delayed the growth of MICA-expressing mouse tumors but not of control tumors. The therapeutic effect of immunization with BLS-MICA included scavenging of sMICA and the anti-MICA Ab-mediated ADCC, promoting heightened intratumoral M1/proinflammatory macrophage and antigen-experienced CD8+T cell recruitment.ConclusionsImmunization with the chimeric protein BLS-MICA constitutes a useful way to actively induce therapeutic anti-MICA pAb that resulted in a reprogramming of the antitumor immune response towards an antitumoral/proinflammatory phenotype. Hence, the BLS-MICA chimeric protein constitutes a novel antitumor vaccine of potential application in patients with MICA-expressing tumors.
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Gomi, Katsushige, Eiji Kobayashi, Katsunori Miyoshi, Tadashi Ashizawa, Akihiko Okamoto, Tatsuhiro Ogawa, Shigeo Katsumata, Akira Mihara, Masami Okabe, and Tadashi Hirata. "Anticellular and Antitumor Activity of Duocarmycins, Novel Antitumor Antibiotics." Japanese Journal of Cancer Research 83, no. 1 (January 1992): 113–20. http://dx.doi.org/10.1111/j.1349-7006.1992.tb02360.x.

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10

Zhang, Lingbing, Dongdong Feng, Lynda X. Yu, Kangla Tsung, and Jeffrey A. Norton. "Preexisting antitumor immunity augments the antitumor effects of chemotherapy." Cancer Immunology, Immunotherapy 62, no. 6 (April 18, 2013): 1061–71. http://dx.doi.org/10.1007/s00262-013-1417-7.

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Dissertations / Theses on the topic "Antitumor"

1

Costa, PatrÃcia MarÃal da. "AvaliaÃÃo do potencial antitumoral dos hidrobenzofuranÃides isolados das folhas da Tapirira guianensis (anacardiaceae)." Universidade Federal do CearÃ, 2006. http://www.teses.ufc.br/tde_busca/arquivo.php?codArquivo=524.

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CoordenaÃÃo de AperfeiÃoamento de Pessoal de NÃvel Superior
Os hidrobenzofuranÃides obtidos da Tapirira guianensis sÃo derivados alquilados da ciclohexanona, que parecem ser possÃveis precursores dos lipÃdios fenÃlicos. O presente trabalho avaliou, inicialmente, a atividade dos nove hidribenzofuranÃides em linhagens de cÃlulas, onde a amostra SJC-8 mostrou a citotoxicidade mais elevada. Posteriormente, foram avaliados os possÃveis mecanismos pelo qual esta amostra desenvolve seu efeito citotÃxico. No teste de MTT em painel de linhagens adicionais a SJC-8 apresentou valores de CI50 variando de 0.3 a 6.2Âg/mL. No teste de toxicidade aguda em nÃuplios de artÃmia e de atividade hemolÃtica em eritrÃcitos de camundongos, a SJC-8 nÃo desenvolveu toxicidade e hemÃlise, respectivamente. O mecanismo de aÃÃo da SJC-8 foi, entÃo, estudado. A viabilidade das cÃlulas HL-60 foi afetada pela SJC-8 apÃs um perÃodo de exposiÃÃo de 24h, quando analisada por exclusÃo por azul de tripan. Nas menores concentraÃÃes nÃo houve aumento do nÃmero de cÃlulas nÃo-viÃveis, mas apenas uma reduÃÃo da proliferaÃÃo celular (aÃÃo citostÃtica), enquanto que nas duas maiores concentraÃÃes, houve reduÃÃo do nÃmero de cÃlulas viÃveis e aumento do nÃmero de cÃlulas nÃo-viÃveis (efeito citotÃxico), o que corrobora com os achados da analise morfolÃgica, onde observou-se um aumento do nÃmero de cÃlulas mortas. A atividade citotÃxica da SJC-8 està relacionada com a inibiÃÃo da sÃntese de DNA, como revelado pela incorporaÃÃo do BrdU, alÃm de poder estar envolvida com a inibiÃÃo da Topoisomerase 1. Submetida ao estudo de toxicogenÃtica pelo teste do cometa em HL-60, a SJC-8 elevou os Ãndices e freqÃÃncias de dano de maneira concentraÃÃo-dependente, sendo observados tipos de danos maiores nas concentraÃÃes mais elevadas. A administraÃÃo de SJC-8 (25 ou 50mg/kg/dia) inibiu o desenvolvimento de tumor sÃlido em camundongos transplantados com Sarcoma 180 em 12,3 e 59,8% respectivamente. A atividade antitumoral da SJC-8 està relacionada com a inibiÃÃo da proliferaÃÃo do tumor. A anÃlise histopatolÃgica mostrou de forma reversÃvel, que o fÃgado à o alvo de toxicidade da droga. De fato, a atividade antitumoral da SJC-8 esta relacionada com um efeito antiproliferativo direto nas cÃlulas tumorais, sendo possÃvel assim que esta amostra possa atuar como possÃvel protÃtipo de novos agentes antitumorais.
The hydrobenzofuranoids obtained from Tapirira guianensis are alkylated derivates of cyclo-hexanone, which appear to be precursors of phenolic lipids. The present study initially examined the activity of nine hydrobenzofuranoids in cell lines, where the compound SJC-8 showed the highest cytotoxicity. In later studies, the cytotoxicity of this sample was investigated with regard to the possible mechanism of action. In the MTT assay, SJC-8 showed IC50 values of 0.3 to 6.2Âg/mL in a panel of cell lines. In acute toxicity assays in artemia nauplii and hemolytic activity in mouse erythrocytes, SJC-8 did not demonstrate any toxicity or hemolysis, respectively. The mechanism of action of SJC-8 was then studied. SJC-8 affected cell viability in HL-60 after an exposure period of 24h, when determined by trypan blue exclusion. At lower concentrations, there was no increase in the number of non-viable cells but only a reduction in cell proliferation (cytostatic effect). However, at the two highest concentrations, there was a decrease in the number of viable cells and increase in number of non-viable cells (cytotoxic effect), which corroborate the findings of morphologic analysis showing an increase in the number of dead cells. The cytotoxicity of SJC-8 involves the inhibition of DNA synthesis, as revealed by inhibition of BrdU incorporation into DNA and of topoisomerase 1 activity. SJC-8 was tested for genotoxicity using the comet assay in HL-60 cells, and was found to cause an increase in the frequency of DNA damage in a concentration-dependent manner, where more severe damage was seen at higher concentrations of SJC-8. The administration of SJC-8 (25 or 50 mg/kg/day) inhibited solid tumor growth in mice transplanted with sarcoma 180, by 12.3 and 59.8%, respectively. The antitumor activity of SJC-8 is attributed to inhibition of tumor cell proliferation. Histopathologic analysis showed in a reversible manner that the liver is the target of drug toxicity. In conclusion, SJC-8 has antitumor activity where it has a direct antiproliferative effect on tumor cells, and may therefore serve as a prototype for new antitumor agents.
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Hill, Gordon Craig. "DNA binding studies of antitumor antibiotics and antitumor anthracene derivatives: Computer simulations and spectrophotometric titrations." Diss., The University of Arizona, 1990. http://hdl.handle.net/10150/185221.

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Quinocarcin binds to d(ATGCAT)₂ with a preferred direction of 3' and the R configuration at C4 of the drug. A mode of action involving ring opening of the oxazolidine ring to form an iminium ion which can then alkylate the N2 of guanine has been reinforced by the current computer modeling study. The absolute configuration for quinocarcin should be reversed based on the fact that the optical isomer of the structure arbitrarily assigned in the literature forms a much better binding complex to DNA. Anthramycin binds to the 2-amino group of guanine but its mechanism of action proceeds through a neutral imine. The 3' direction is again favored but for this molecule, the preferred configuration is S. This computer modeling study provided a basis for a 2D NMR study which confirmed that anthramycin forms a 3'S adduct when it binds to d(ATGCAT)₂. Bisantrene and R9 are synthetic anthracene derivatives with antitumor activity. Use of UV spectroscopy provided insight into the ability of these compounds to intercalate between the base pairs of double helical DNA. Standard Scatchard plot analysis proved useless in determining the binding parameters. A McGhee-von Hippel equation was able to describe a portion of the data but a smoothing spline function was able to describe the data completely. Naphthyridinomycin studies indicate that it too prefers a covalent adduct in which the direction is 3' and the configuration is R at C7. When the noncovalent drug binds to d(ATGCAT)₂ it may bind with either the C3a face or the C7 face closest to N2 of guanine. Iminium ion mechanisms have been proposed for the binding of naphthyridinomycin to N2 of guanine in the minor groove of DNA and the computer modeling presents evidence to support such mechanisms. Saframycin A binds much better to d(GATGCATC)₂ as a hydroquinone species but the quinone can still bind in the same site. The 3' direction is clearly preferred with the R configuration at C7. The hydrogen bonding network of the hydroquinone is conserved in the noncovalent, iminium ion, and covalent 3'R models after 32 ps of dynamics. Iminium ion mechanisms have been proposed for the binding of saframycin A to N2 of guanine in the minor groove of DNA and the computer modeling presents evidence to support such mechanisms.
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Mokdsi, George. "Antitumour Metallocenes." Thesis, The University of Sydney, 2000. http://hdl.handle.net/2123/794.

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This thesis reports a study of the chemical stability and coordination chemistry of several antitumour metallocenes Cp2MCl2 (Cp = h5-C5H5; M = Ti 1, V 2, Nb 3, Mo 4), as well as derivatives of Cp2TiCl2 1, with nucleic acids, nucleic acid constituents and proteins. These studies were carried out in order to identify the biologically active species and more fully understand the molecular level mechanism of action of the antitumour metallocenes, in particular Cp2TiCl2 1, which is currently undergoing phase II clinical trials. The interactions of Cp2MoCl2 4 with four oligonucleotides were studied by 1H and 31P NMR spectroscopy. In 50 mM salt solutions of Cp2MoCl2 4, hydrolysis of the halide ligands occurred to give a solution with pD -2, containing a species in which both Cp rings remain metal bound for 24 h. At pD -7, partial hydrolysis of the Cp rings (-30percent) occurred after 24 h. Addition of an aqueous solution of Cp2MoCl2 4 in 50 mM salt to the self-complementary sequence d(CGCATATGCG)2, maintaining the pD at 6.0-7.0, showed no evidence for the formation of a metallocene-oligonucleotide complex and only peaks arising from hydrolysis of Cp2MoCl2 4 were detected. A similar result was obtained in titration experiments with the single stranded sequence d(ATGGTA) at pD 6.5-7.0. However, at pD 3.0, new signals assigned to a molybdocene-oligonucleotide complex(es), which was stable for hours at pD 3.0, were detected; while at pD -7 the complex is destabilised and only peaks arising from hydrolysis of Cp2MoCl2 4 were detected. Titration experiments at low pD with Cp2MoCl2 4 and the dinucleotide dCG were consistent with formation of a complex arising due to coordination of molybdenum to guanine N7 and/or cytosine N3. The results obtained showed that stable oligonucleotide adducts were not formed in 50 mM salt at pD -7 and hence it is highly unlikely that formation of molybdocene-DNA adducts in vivo is the primary action that is responsible for the antitumour properties of Cp2MoCl2 4. The rate of hydrolysis of the aromatic rings of Cp2TiX2 (X equals Cl 1, OCOCH2NH3Cl 27) and the dimethylsubstituted derivatives (MeCp)2TiX2 (X equals Cl 34, OCOCH2NH3Cl 41), in aqueous solutions at pD 2-8 was studied by 1H NMR spectroscopy. Rapid hydrolysis of both the halide/glycine and Cp ligands in Cp2TiX2 (X equals Cl 1, OCOCH2NH3Cl 27) occurred and predominantly gave a precipitate at pD -7. In contrast, under the same experimental conditions, the predominant species present in aqueous solutions of (MeCp)2TiX2 (X equals Cl 34, OCOCH2NH3Cl 41) at pH 2-8 contained both MeCp rings metal bound. At pD < 5, Cp2TiX2 (X equals Cl 1, OCOCH2NH3Cl 27) and (MeCp)2TiX2 (X equals Cl 34, OCOCH2NH3Cl 41) formed similar complex(es) with purine nucleotides. However, at pD >5, stable adducts between nucleotides and Cp2TiX2 (X equals Cl 1, OCOCH2NH3Cl 27) were not formed. In contrast, (MeCp)2TiX2 (X equals Cl 34, OCOCH2NH3Cl 41) formed complex(es) with 5'-dAMP or 5'-dGMP, which were stable for 24 h. These results suggest that formation of stable chelates between (MeCp)2TiX2 (X equals Cl 34, OCOCH2NH3Cl 41) and nucleic acid constituents in vivo is possible. However, the methyl substituted derivatives 34 and 41 did not show any antitumour activity against EAT in mice when administered in either 10percentDMSO/90percentsaline or in water at pH 6.2-6.4, which suggests that the labile Cp-Ti bond present in Cp2TiCl2 1 is required for antitumour activity. The synthesis of a range of Cp substituted titanocene derivatives was investigated in an attempt to prepare derivatives with modified Cp stability in comparison to the methyl substituted derivatives. The synthesis of derivatives (CpCH2Y)2TiCl2 where Y equals ?CHO 43, ?CONMe2 44, ?NO2 45, (RCp)2TiCl2 where R equals ?COMe 46, ?COOMe 47 or ?CONMe2 48, (CpNMe2)2TiCl2 62 and (Cp(CH2)2NMe2)2TiCl2 63 was unsuccessful, due to the presence of coordinating substituents on the Cp rings and poor stability in polar, protic solvents. Hence, these derivatives were excluded from further studies. The rate of hydrolysis of the Cp rings of Cp2TiX2 (X equals Cl 1, OCOCCl3 22 and OCOCH2NH3Cl 27) in aqueous solutions, 10percentDMSO/90percentD2O and 100percent DMSO was monitored by 1H NMR spectroscopy. Rapid hydrolysis of both the carboxylate and Cp ligands of Cp2TiX2 (OCOCCl3 22 and OCOCH2NH3Cl 27) occurred in DMSO to give biologically inactive species. The rate of these reactions were concentration dependent as dilution of these samples with saline or water to give the therapeutic conditions of 10percentDMSO/90percentD2O slowed the hydrolysis chemistry. In contrast, samples of Cp2TiX2 (X equals Cl 1 and OCOCH2NH3Cl 27) dissolved in water, gave solutions containing the presumed antitumour active species in which the halide or glycine ligands have been hydrolysed but the Cp rings remain metal bound. Thus, charged X ligands may be incorporated into Cp2TiX2 and will give comparable activity to Cp2TiCl2 1 provided the samples are administered in water. The antitumour metallocenes Cp2MCl2 (M equals Ti 1, V 2, Nb 3, Mo 4) and the inactive derivative (MeCp)2TiCl2 34 were found to inhibit the relaxation of supercoiled plasmid DNA pBR322 by human topoisomerase II in vitro. These results implicated the inhibition of topoisomerase II in the mechanism of antitumour activity although there was no direct correlation between the in vitro results with biological activity against EAT in vivo. UV spectroscopy confirmed that the metallocenes Cp2MCl2 (M equals Ti 1, Mo 4) became associated with and were stabilised to hydrolysis by calf thymus DNA but not with human serum albumin. ICP-AES was used to measure the amount of metal associated with either DNA or human serum albumin after incubation with Cp2MCl2 (M equals Ti 1, Nb 3, Mo 4) and dialysis of these solution. The results confirmed that DNA stabilises or becomes associated with the metallocenes. However, errors associated with the ICP-AES measurements did not allow these results to be quantified. 1H NMR spectroscopy was used to show that the antitumour metallocene Cp2MoCl2 4 formed an adduct with glutathione 72 in the pH range 3-7 through the sulfur donor group. In comparison, the antitumour metallocenes Cp2MCl2 (M equals Ti 1, Nb 3) showed limited adduct formation with glutathione 72 at pH -3 and no adducts were detected at pH > 5.5.
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Mokdsi, George. "Antitumour Metallocenes." University of Sydney. Chemistry, 2000. http://hdl.handle.net/2123/794.

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This thesis reports a study of the chemical stability and coordination chemistry of several antitumour metallocenes Cp2MCl2 (Cp = h5-C5H5; M = Ti 1, V 2, Nb 3, Mo 4), as well as derivatives of Cp2TiCl2 1, with nucleic acids, nucleic acid constituents and proteins. These studies were carried out in order to identify the biologically active species and more fully understand the molecular level mechanism of action of the antitumour metallocenes, in particular Cp2TiCl2 1, which is currently undergoing phase II clinical trials. The interactions of Cp2MoCl2 4 with four oligonucleotides were studied by 1H and 31P NMR spectroscopy. In 50 mM salt solutions of Cp2MoCl2 4, hydrolysis of the halide ligands occurred to give a solution with pD -2, containing a species in which both Cp rings remain metal bound for 24 h. At pD -7, partial hydrolysis of the Cp rings (-30percent) occurred after 24 h. Addition of an aqueous solution of Cp2MoCl2 4 in 50 mM salt to the self-complementary sequence d(CGCATATGCG)2, maintaining the pD at 6.0-7.0, showed no evidence for the formation of a metallocene-oligonucleotide complex and only peaks arising from hydrolysis of Cp2MoCl2 4 were detected. A similar result was obtained in titration experiments with the single stranded sequence d(ATGGTA) at pD 6.5-7.0. However, at pD 3.0, new signals assigned to a molybdocene-oligonucleotide complex(es), which was stable for hours at pD 3.0, were detected; while at pD -7 the complex is destabilised and only peaks arising from hydrolysis of Cp2MoCl2 4 were detected. Titration experiments at low pD with Cp2MoCl2 4 and the dinucleotide dCG were consistent with formation of a complex arising due to coordination of molybdenum to guanine N7 and/or cytosine N3. The results obtained showed that stable oligonucleotide adducts were not formed in 50 mM salt at pD -7 and hence it is highly unlikely that formation of molybdocene-DNA adducts in vivo is the primary action that is responsible for the antitumour properties of Cp2MoCl2 4. The rate of hydrolysis of the aromatic rings of Cp2TiX2 (X equals Cl 1, OCOCH2NH3Cl 27) and the dimethylsubstituted derivatives (MeCp)2TiX2 (X equals Cl 34, OCOCH2NH3Cl 41), in aqueous solutions at pD 2-8 was studied by 1H NMR spectroscopy. Rapid hydrolysis of both the halide/glycine and Cp ligands in Cp2TiX2 (X equals Cl 1, OCOCH2NH3Cl 27) occurred and predominantly gave a precipitate at pD -7. In contrast, under the same experimental conditions, the predominant species present in aqueous solutions of (MeCp)2TiX2 (X equals Cl 34, OCOCH2NH3Cl 41) at pH 2-8 contained both MeCp rings metal bound. At pD < 5, Cp2TiX2 (X equals Cl 1, OCOCH2NH3Cl 27) and (MeCp)2TiX2 (X equals Cl 34, OCOCH2NH3Cl 41) formed similar complex(es) with purine nucleotides. However, at pD >5, stable adducts between nucleotides and Cp2TiX2 (X equals Cl 1, OCOCH2NH3Cl 27) were not formed. In contrast, (MeCp)2TiX2 (X equals Cl 34, OCOCH2NH3Cl 41) formed complex(es) with 5'-dAMP or 5'-dGMP, which were stable for 24 h. These results suggest that formation of stable chelates between (MeCp)2TiX2 (X equals Cl 34, OCOCH2NH3Cl 41) and nucleic acid constituents in vivo is possible. However, the methyl substituted derivatives 34 and 41 did not show any antitumour activity against EAT in mice when administered in either 10percentDMSO/90percentsaline or in water at pH 6.2-6.4, which suggests that the labile Cp-Ti bond present in Cp2TiCl2 1 is required for antitumour activity. The synthesis of a range of Cp substituted titanocene derivatives was investigated in an attempt to prepare derivatives with modified Cp stability in comparison to the methyl substituted derivatives. The synthesis of derivatives (CpCH2Y)2TiCl2 where Y equals ?CHO 43, ?CONMe2 44, ?NO2 45, (RCp)2TiCl2 where R equals ?COMe 46, ?COOMe 47 or ?CONMe2 48, (CpNMe2)2TiCl2 62 and (Cp(CH2)2NMe2)2TiCl2 63 was unsuccessful, due to the presence of coordinating substituents on the Cp rings and poor stability in polar, protic solvents. Hence, these derivatives were excluded from further studies. The rate of hydrolysis of the Cp rings of Cp2TiX2 (X equals Cl 1, OCOCCl3 22 and OCOCH2NH3Cl 27) in aqueous solutions, 10percentDMSO/90percentD2O and 100percent DMSO was monitored by 1H NMR spectroscopy. Rapid hydrolysis of both the carboxylate and Cp ligands of Cp2TiX2 (OCOCCl3 22 and OCOCH2NH3Cl 27) occurred in DMSO to give biologically inactive species. The rate of these reactions were concentration dependent as dilution of these samples with saline or water to give the therapeutic conditions of 10percentDMSO/90percentD2O slowed the hydrolysis chemistry. In contrast, samples of Cp2TiX2 (X equals Cl 1 and OCOCH2NH3Cl 27) dissolved in water, gave solutions containing the presumed antitumour active species in which the halide or glycine ligands have been hydrolysed but the Cp rings remain metal bound. Thus, charged X ligands may be incorporated into Cp2TiX2 and will give comparable activity to Cp2TiCl2 1 provided the samples are administered in water. The antitumour metallocenes Cp2MCl2 (M equals Ti 1, V 2, Nb 3, Mo 4) and the inactive derivative (MeCp)2TiCl2 34 were found to inhibit the relaxation of supercoiled plasmid DNA pBR322 by human topoisomerase II in vitro. These results implicated the inhibition of topoisomerase II in the mechanism of antitumour activity although there was no direct correlation between the in vitro results with biological activity against EAT in vivo. UV spectroscopy confirmed that the metallocenes Cp2MCl2 (M equals Ti 1, Mo 4) became associated with and were stabilised to hydrolysis by calf thymus DNA but not with human serum albumin. ICP-AES was used to measure the amount of metal associated with either DNA or human serum albumin after incubation with Cp2MCl2 (M equals Ti 1, Nb 3, Mo 4) and dialysis of these solution. The results confirmed that DNA stabilises or becomes associated with the metallocenes. However, errors associated with the ICP-AES measurements did not allow these results to be quantified. 1H NMR spectroscopy was used to show that the antitumour metallocene Cp2MoCl2 4 formed an adduct with glutathione 72 in the pH range 3-7 through the sulfur donor group. In comparison, the antitumour metallocenes Cp2MCl2 (M equals Ti 1, Nb 3) showed limited adduct formation with glutathione 72 at pH -3 and no adducts were detected at pH > 5.5.
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SOUZA, Pâmella Grasielle Vital Dias de. "Avaliação da ação antitumoral de Cnidoscolus urens sobre tumores sólidos experimentais em camundongos Swiss." Universidade Federal de Pernambuco, 2013. https://repositorio.ufpe.br/handle/123456789/16728.

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Cnidoscolus urens pertence à família das Euphorbiaceae que é considerada uma das seis maiores famílias de Gimnospermas do bioma Caatinga. Esta espécie conhecida popularmente como urtiga branca, em levantamentos etnobotânicos realizados com populares da região do Nordeste, aparece com boa frequência e com o relato de diversas atividades biológicas como anti-inflamatória, antitumoral, antimicrobiana e analgésica. Portanto esta dissertação teve como objetivo, determinar o perfil fitoquímico dos extratos aquoso, N- butanólico e acetato de etila de C. urens, a atividade in vitro dos extratos aquoso e etanólico de C. urens e atividade antitumoral in vivo dos mesmos extratos de C. urens frente à linhagem celular HELA. Assim, para avaliar a eficácia das atividades descritas pela população, iniciou- se a investigação dos constituintes metabólitos secundários produzidos por C. urens através do método de cromatografia de camada delgada (CCD). A citotoxicidade foi determinada pelo método de MTT e para a determinação da atividade antitumoral in vivo, foram induzidos carcinoma de Ehrlich experimentais em camundongos Swiss, a determinação do perfil hematológico foi obtida através de contagem automática das células vermelhas e o perfil bioquímico foi determinado por métodos enzimáticos. Os extratos aquoso, N- butanólico e acetato de etila revelaram a presença de metabólitos majoritários tais como: Flavonóides, açúcares redutores e terpenóidess, além de outros compostos como cumarinas e taninos que apresentaram- se em menor concentração. Os extratos aquoso e etanólico foram efetivos na inibição do crescimento do tumor sólido de carcinoma de Ehrlich (84.4% e 79.2%, respectivamente) inclusive melhorando os parâmetros bioquímicos, sendo mantidos os níveis de ureia, creatinina, colesterol total, HDL-colesterol, glicose e triglicerídios e hematológicos para células sanguíneas vermelhas, células brancas e hemoglobina, indicando uma melhora na resposta imunológica dos animais tratados com os extratos. Os extratos aquoso e etanólico de C. urens não mostraram toxicidade in vitro frente à células HELA, nas concentrações testadas 12,5; 25; 50 e 100 μg/ mL, no entanto, apresentaram potencial antioxidante >50% para as concentrações de 50; 100; 200 e 500 μg/ mL. Diante desses resultados podemos concluir que os extratos aquosos e etanólico C. urens foram eficazes em inibir o crescimento do tumoral.
Cnidoscolus urens belongs to the family Euphorbiaceae which is considered one of the six largest families of gymnosperms of biome Caatinga from Brazil. This species are commonly known as urtiga branca and appears with good frequency and reporting of various biological activities such as anti-inflammatory, antitumor, antibacterial and analgesic in ethnobotanical surveys conducted in Northeast region. Therefore, this thesis aimed to determine the phytochemical profile of aqueous, butanolic and ethyl acetate of C. urens and in vivo antitumoral activity of aqueous and ethanolic extracts of C. urens and in vitro cytotoxic activity of same extracts C. urens in Hela cell line. Thus, to assess the efficacy of proposed activities for this work, it was started the research of metabolites produced by C. urens by thin layer chromatography (TLC) method, cytotoxicity was determined by the MTT method and solid tumors were induced in mice to determine the in vivo antitumoral activity, blood sampling at the orbital plexus was conducted in order to perform hematological and biochemical profile by automated cell count and enzymatic methods, respectively. The aqueous extracts, butanolic and ethyl acetate, revealed the presence of major metabolites such as flavonoids, terpenes and reducing sugars, and other compounds such as coumarins and tannins that are present in lower concentrations. The aqueous and ethanolic extracts were effective in inhibiting tumor growth (84.4% and 79.2%, respectively) and also improving biochemical (maintenance of urea, creatinine, total cholesterol, HDL-cholesterol, triglycerides and glucose levels) and hematologic parameters (red blood cells, white blood cells and hemoglobin), which indicate an improvement of the immune response of animals treated with the extracts. The aqueous and ethanolic extracts of C. urens showed no toxicity in vitro against the Hela cells, otherwise, they showed potential antioxidant activity higher than 50% at concentrations of 50, 100, 200 and 500 mg/mL. From these results we conclude that the aqueous and ethanol extracts of Cnidoscolus urens were effective in inhibiting the growth of Ehrlich tumor models of solids.
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GONÇALVES, Joelma Pessoa. "Avaliação da citotoxicidade e genotoxicidade de extratos orgânicos e ácido barbático isolado do líquen Cladonia salzmannii (Nyl.)." Universidade Federal de Pernambuco, 2015. https://repositorio.ufpe.br/handle/123456789/17320.

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Os metabólitos secundários dos liquens são responsáveis pela maioria das suas atividades biológicas. Muitos destes compostos apresentam relevante atividade antineoplásica. O objetivo deste trabalho foi verificar as atividades citotóxica e genotóxica in vitro dos extratos orgânicos e do ácido barbático (BAR) purificado de Cladonia salzmannii Nyl. Os extratos orgânicos foram obtidos a partir do talo liquênico (22 g) previamente limpo e seco, com os solventes éter dietílico, clorofórmio e acetona, através do método de esgotamento a quente em aparelho de Soxhlet. O ácido barbático foi purificado a partir do extrato etéreo (1,3 g). A análise química dos extratos orgânicos e do BAR purificado foi realizada através de Cromatografia em Camada Delgada (CCD). A pureza do BAR purificado foi observada através de Cromatografia Líquida de Alta Eficiência (CLAE). A atividade citotóxica dos extratos orgânicos e do BAR purificado foi determinada através do Método do MTT [brometo de 3-(4,5-dimetiltiazol-2-il)-2,5-difeniltetrazólio] e do IPBC (Índice de Proliferação com Bloqueio da Citocinese). O potencial genotóxico dos extratos orgânicos e do BAR purificado foram determinados através do teste do micronúcleo e do ensaio cometa. O dimetilsulfoxido (DMSO) foi utilizado como solvente de diluição das amostras em todos os testes de atividade biológica. Os resultados referentes a CI50 demonstraram relevante potencial citotóxico para o extrato etéreo (Ext E) (50 μg/mL) frente as linhagens celulares NCI-H292 (CI50: 29,91 μg/mL), HEp-2 (CI50: 26,75 μg/mL) e HL-60 (CI50: 3,59 μg/mL), e para o BAR purificado (25 μg/mL) contra as linhagens HEp-2 (CI50: 15,79 μg/mL) e MCF-7 (CI50: 18,28 μg/mL). Porém, a avaliação da citotoxicidade considerando o Índice de Proliferação com Bloqueio de Citocinese (IPBC) demonstrou atividade citotóxica para o BAR purificado em todas as concentrações testadas (5, 10, 20 e 40 μg/mL) e para todos os extratos orgânicos (50 μg/mL) frente as células do Carcinoma de Ehrlich. Entretanto, para o Sarcoma 180 apenas o BAR purificado na concentração de 40 μg/mL e os extratos etéreo e clorofórmico (50 μg/mL) foram considerados citotóxicos. O teste do micronúcleo (MN) demonstrou que o BAR purificado na concentração de 5 μg/mL não apresentou potencial genotóxico em ambas as linhagens celulares tumorais. Além disso, o extrato clorofórmico e BAR purificado na concentração de 10 μg/mL não foram considerados genotóxicos para o Sarcoma 180. No ensaio cometa, todos os compostos testados induziram danos ao DNA em ambas as linhagens tumorais. Com base nos resultados, considera-se que os extratos orgânicos e o BAR purificado de C. salzmannii (Nyl). apresentam atividade citotóxica e genotóxica frente as linhagens celulares tumorais testadas.
The secondary metabolites of lichens are responsible for most of their biological activities. Many of these compounds exhibit significant antineoplastic activity. The objective of this study was to evaluate the in vitro cytotoxic and genotoxic activities of organic extracts and purified barbatic acid from Cladonia salzmannii Nyl. The organic extracts were obtained from liquenic thallus (22 g) previously cleaned and dried with the solvents diethyl ether, chloroform and acetone, through hot exhausted method in a Soxhlet apparatus. The barbatic acid was purified from the ether extract (1.3 g). Chemical analysis of the organic extracts and purified BAR was performed by Thin Layer Chromatography (TLC). The purity of purified BAR was observed by High Performance Liquid Chromatography (HPLC). The cytotoxic activity of the organic extracts and purified BAR was determined by the MTT method [3-(4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide] and IPBC (Cytokinesis-Block Proliferation Index). The genotoxic potential of the organic extracts and purified BAR was determined by the micronucleus test and comet assay. Dimethyl sulfoxide (DMSO) was used as diluting solvent of the samples in all biological tests. The results for IC50 demonstrated significant cytotoxic potential to the ether extract (Ext E) (50 μg/mL) against the cell lines NCI-H292 (IC50: 29,91 μg/mL), HEp-2 (IC50: 26,75 μg/mL) and HL-60 (IC50: 3,59 μg/mL) and to the purified BAR (25 μg/mL) against the cell lines HEp-2 (IC50: 15,79 μg/mL) and MCF-7 (IC50: 18,28 μg/mL). However, the assessment of cytotoxicity considering the Cytokinesis-Block Proliferation Index (IPBC) showed cytotoxic activity for purified BAR at all concentrations tested (5, 10, 20 and 40 μg/mL) and for all organic extracts (50 μg/mL) against Ehrlich carcinoma cells. However, for Sarcoma 180 only BAR purified at a concentration of 40 μg/mL and ether and chloroform extracts (50 μg/mL) were considered cytotoxic. The micronucleus test (MN) showed that the purified BAR at a concentration of 5 μg/mL showed no genotoxic potential in both tumor cell lines. Furthermore, the chloroform extract and purified BAR at a concentration of 10 μg/mL were not considered genotoxic for Sarcoma 180. In the comet assay, all compounds tested induced DNA damage in both tumor lines. Based on the results, it is considered that the organic extracts and the BAR purified from C. salzmannii (Nyl). exhibit cytotoxic and genotoxic activity front of the tested tumor cell lines.
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Loch, Rebecca [Verfasser], and Georg [Akademischer Betreuer] Bauer. "Antimikrobielle Wirkstoffe als potenzielle Antitumor- Mittel." Freiburg : Universität, 2015. http://d-nb.info/1119452147/34.

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Loch, Rebecca. "Antimikrobielle Wirkstoffe als potenzielle Antitumor-Mittel." [S.l. : s.n.], 2007. http://nbn-resolving.de/urn:nbn:de:bsz:25-opus-49014.

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Mousinho, Kristiana Cerqueira. "Estudo do Potencial AnticÃncer de um Derivado de Chalcona, 1-(4-Nitrofenil)-3-Fenilprop-2-En-1-Ona, In vitro e In vivo." Universidade Federal do CearÃ, 2010. http://www.teses.ufc.br/tde_busca/arquivo.php?codArquivo=10509.

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CoordenaÃÃo de AperfeiÃoamento de NÃvel Superior
A substÃncia 1-(4-Nitrofenil)-3-fenilprop-2-en-1-ona (CG) Ã um derivado de chalcona, sintetizado a partir da reaÃÃo quÃmica entre a acetofenona e para-nitro benzaldeÃdo. Para avaliar o seu potencial anticÃncer foi realizado um estudo farmacolÃgico de suas propriedades antitumorais em vÃrios modelos biolÃgicos in vitro e in vivo. A CG apresentou potente atividade citotÃxica nas 5 linhagens tumorais testadas, inibindo a proliferaÃÃo das cÃlulas tumorais pelo ensaio do MTT e em cÃlulas mononucleares do sangue perifÃrico (PMCB) humano atravÃs do ensaio do Alamar blue. Todas as linhagens mostraram sensibilidade ao tratamento com a CG, e a CI50 variou de 1,18ÂM em HCT-8 a 3,32ÂM em SF-295. O composto apresentou fraca citotoxicidade (CI50 igual a 7,07ÂM) nas cÃlulas PBMC, com exposiÃÃo a CG em 72h, em relaÃÃo Ãs cÃlulas de HL-60, utilizada como modelo nos demais testes biolÃgicos. O tempo de encubaÃÃo com o composto foi de 24h na maioria dos experimentos. Adicionalmente, a CG nÃo induziu efeitos hemolÃticos. O ensaio de exclusÃo por azul de Tripan revelou diminuiÃÃo da viabilidade celular principalmente apÃs 24h na maior concentraÃÃo testada (4ÂM) com 58,4%. Para os testes de atividade antiproliferativa, LA/BE mostrou em sua morfologia cÃlulas em apoptose nas duas maiores concentraÃÃes, enquanto que o BrdU, apresentou incorporaÃÃo do mesmo nas concentraÃÃes testadas. A morfologia analisada por May-Grunwald-Giemsa mostrou reduÃÃo do volume celular, condensaÃÃo da cromatina e fragmentaÃÃo nuclear. Adicionalmente, a CG induziu apoptose em cÃlulas leucÃmicas HL-60, com participaÃÃo das vias intrÃnseca e maior estÃmulo da via extrÃnseca, de maneira concentraÃÃo-dependente, como observado na integridade da membrana citoplasmÃtica, aumento da fragmentaÃÃo do DNA e externalizaÃÃo da fosfatidilserina. Na anÃlise do ciclo celular, foi observado parada na fase G2/M, sendo ativada as caspases 3, 7, 8 e 9 (a Ãltima na maior concentraÃÃo e confirmada pelo teste do Western blot). NÃo houve ativaÃÃo do Citocromo c. A CG nÃo foi capaz de induzir processos genotÃxicos/ mutagÃnicos (testes do cometa e micronÃcleo in vitro). No ensaio de atividade antitumoral in vivo, observou-se inibiÃÃo tumoral nas doses testadas (25 e 50mg/Kg/dia, via oral) de 54,85 e 69,11% respectivamente. As doses de CG causaram tumefaÃÃo celular e o surgimento de focos inflamatÃrios no parÃnquima ou estroma hepÃtico/renal, necrose nefrotÃxica focal, esteatose microvesicular, pigmentos de hemossiderina, hiperplasia das cÃlulas de Kupffer, congestÃo da polpa vermelha e desorganizaÃÃo dos folÃculos linfÃides esplÃnicos. AlÃm disso, os Ãndices bioquÃmicos mostraram aumento do AST e diminuiÃÃo da urÃia (CG 25mg/Kg/dia), diminuiÃÃo do ALT (5-FU e CG 25mg/Kg/dia); as alteraÃÃes hematolÃgicas mostraram leucopenia e plaquetopenia (5-FU), aumento dos leucÃcitos totais (CG 50mg/Kg/dia), aumento de neutrÃfilos e linfÃcitos em todos os grupos tratados. Todos os resultados nos levam a enfatizar que a CG possui grande potencialidade como molÃcula promissora por suas propriedades anticÃncer.
The substance 1- (4-Nitrofenil)-3- fenilprop-2- en-1-ona (CG) is a chalcone derivative, synthesized from a chemical reaction between acetophenone and p-nitro benzaldehyde. To evaluate its anticancer potential a pharmacological study of its antitumor properties in selected biological models in vitro e in vivo. CG presented a powerful cytotoxic activity in the 5 tested tumor lines evaluated, inhibiting cell proliferation of the tumor lines in the MTT assay and human peripheral mononuclear blood cells (PMBC) through the Alamar Blue assay. All cell lines showed sensitivity to the treatment with the CG, and the IC50 varied from 1,18 ÂM in HCT-8 to 3,32 ÂM in SF-295. The sample presented weak cytotoxic effect (IC50 of 7,07 ÂM) in cells PMBC, with 72h exposure to CG, compared to HL-60 cells (leukemic cell line), used in the next biological tests. The sample was incubated with the cells during 24h for the majority of the experiments. Additionally, CG did not induce hemolytic effects. The Tripan Blue assay showed a decrease of the cellular viability especially after 24h of incubation of the higher tested concentration (4 ÂM) with 58,4%. In assays for antiproliferative activity, OA/BE showed in its morphology cells going under apoptosis in the two higher concentrations, whereas the BrdU assay, presented incorporation of the same in the tested concentrations. The morphology analyzed with the May-Grunwald-Giemsa stain showed a decrease of the cellular volume, chromatin condensation and nuclear fragmentation.CG induced apoptosis in HL-60 cells, with participation of the intrinsic pathway and major stimulation of the extrinsic pathway, in a concentration-dependent manner, as observed in the cytoplasmatic membrane integrity, increase of DNA fragmentation and outsourcing of phosphatidylserine. In the cellular cycle analysis, it was observed a stop in the G2/M phase, activating caspases 3, 7, 8 and 9 (the last one in the highest concentration and confirmed by the Western blot assay). It was not observed activation of Cytochrome c. CG was not capable to induce mutagenic/genotoxic processes (comet assay and micronucleus in vitro). In the in vivo antitumor activity assay, tumor inhibition was observed in the tested doses (25 and 50mg/Kg/day, oral intake) of 54,85 and 69,11%, respectively . The doses of CG caused cellular swelling and the arise of inflammatory focus in the parenchyma or hepatic/renal stroma, focal nephrotoxic necrosis, microvesicular steatosis, hemosiderin pigments, hyperplasia of Kupffer cells, congestion of the red pulp and disorganization of the splenic lymphoid follicles. Furthermore, the biochemical indices had shown increase of AST and reduction of urea (25mg/Kg/day of CG), reduction of ALT (25mg/Kg/day of 5-FU and CG); hematologic alterations showed leukopenia and thrombocytopenia (5-FU), increase of total leukocytes (50mg/Kg/day of CG), increase of neutrophils and lymphocytes in all treated groups. All results led us to emphasize that CG possesses great potential as a promising molecule for its anticancer properties.
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Trazzi, Giordano. "Sintese de lignanas a partir de adutos de Morita-Baylis-Hillman : uma via geral de acesso a lignanas biologicamente ativas." [s.n.], 2008. http://repositorio.unicamp.br/jspui/handle/REPOSIP/250252.

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Orientador: Fernando Antonio Santos Coelho
Tese (doutorado) - Universidade Estadual de Campinas, Instituto de Química
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Resumo: Lignanas são produtos naturais produzidos por plantas, cuja diversidade estrutural e pronunciada atividade biológica têm atraído o interesse acadêmico e industrial há mais de um século, a exemplo do fármaco antitumoral Etoposide® (Sandoz), derivado semi-sintético da podofilotoxina, uma lignana natural até hoje comercialmente obtida por extração vegetal. Dentre as rotas de síntese de lignanas, as mais eficazes empregam uma b-benzil-g-butirolactona como intermediário-chave da estratégia. Nesse contexto, propusemos o emprego da reação de Morita-Baylis-Hillman (MBH) para o preparo de a-(aril-hidroximetil)- acrilatos (adutos de MBH) e sua utilização como materiais de partida para a síntese de b-(aril-silaniloximetil)-g-butirolactonas, novos intermediários-chave para a síntese de lignanas. Partindo paralelamente do piperonal, do 6-bromo-piperonal e da vanilina, empregamos a reação de MBH para preparar os a-(aril-hidroximetil)- acrilatos correspondentes, e então os utilizamos na preparação de suas respectivas b-(aril-silaniloximetil)-g-butirolactonas, de forma diastereosseletiva e com rendimentos globais de 56% a 69%, em 4 etapas a partir dos adutos de MBH. A b-(piperonil-silaniloximetil)-g-butirolactona foi empregada com alta eficiência na síntese total das lignanas naturais (±)-yateína, (±)-podorrizol e (±)-epi-podorrizol. A b-(6-bromo-piperonil-silaniloximetil)-g-butirolactona permitiu a preparação de um intermediário avançado para uma nova proposta sintética para a (±)- podofilotoxina. A b-(guaiacil-silaniloximetil)-g-butirolactona, obtida a partir da vanilina, e um intermediário chave para a síntese racemica da porção aglicona do medusasídeo A, uma nova lignana da classe dos dibenzilbutanodiois, cuja síntese ainda não foi descrita
Abstract: Lignans are plant-produced natural products, which structural diversity and pronounced biological activity has being attracting the interest of academy and industry through the entire last century, taking as example the antineoplasic drug Etoposide® (Sandoz), a semi-synthetic derivative of podophyllotoxin, a natural lignan which is, up to date, commercially obtained only by vegetal extraction. Among the routes of synthesis to lignans, the most efficient ones uses a b-benzyl- g-butyrolactone as the key intermediate. In this scenario, we have envisaged the use of the Morita-Baylis-Hillman reaction to synthetize a-(aryl-hydroxymethyl)- acrylates (MBH adducts) and it¿s use as starting materials to the synthesis of b-(aryl-silanyloxymethyl)-g-butyrolactones, new key intermediates to the synthesis of lignans. Starting alongside from piperonal, b-bromo-piperonal and vanillin, we used the MBH reaction to prepare the corresponding a-(aryl-hydroxymethyl)-acrylates (MBH adducts), and used it in the preparation of it¿s corresponding b-(arylsilanyloxymethyl)- g-butyrolactones, in a diastereoselective way and with global yields from 56% to 69% in four steps. The b-(piperonyl-silanyloxymethyl)-g- butirolactone obtained was used with high efficiency in the synthesis of natural lignans (±)-yatein, (±)-podorrizol and (±)-epi-podorrizol. The b-(6-bromo-piperonylsilanyloxymethyl)- g-butirolactone obtained allowed the preperation of an advanced intermediate to a new synthetic strategy to (±)-podophyllotoxyn. The b-(guaiacylsilanyloxymethyl)- g-butirolactone obtained is a key intermediate to the racemic synthesis of medusaside A aglycone, a new dibenzylbutanediol lignan whose synthesis was not described yet
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Quimica Organica
Doutor em Ciências
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Books on the topic "Antitumor"

1

Antitumor steroids. San Diego: Academic Press, 1992.

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Lee, Moses, ed. Heterocyclic Antitumor Antibiotics. Berlin, Heidelberg: Springer Berlin Heidelberg, 2006. http://dx.doi.org/10.1007/11413073.

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T, Hill Bridget, and Bellamy Angela S, eds. Antitumor drug-radiation interactions. Boca Raton, Fla: CRC Press, 1990.

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Muggia, Franco M., and Marcel Rozencweig, eds. Clinical Evaluation of Antitumor Therapy. Boston, MA: Springer US, 1987. http://dx.doi.org/10.1007/978-1-4613-2317-4.

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Working group on molecular mechanisms of carcinogenic and antitumor activity (Città del Vaticano 1986). Molecular mechanisms of antitumor activity. Città del Vaticano: Pontificia Academia Scientiarum, 1987.

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1932-, Borders Donald B., and Doyle Terrence W. 1942-, eds. Enediyne antibiotics as antitumor agents. New York: M. Dekker, 1995.

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Parshikov, Igor A. Features of Antitumor and Antimalarial Artemisinins Biotransformations. Dallas, USA: Primedia E-launch LLC, 2018.

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1923-, Takeuchi Tomio, Nitta Kazuo, Tanaka Nobuo 1926-, Umezawa Hamao, and Nihon Gan Gakkai, eds. Antitumor natural products: Basic and clinical research. Tokyo: Japan Scientific Societies Press, 1989.

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Maran, Carmen. Discovery and development of anthracycline antitumor antibiotics. Timisoara: Universitatea din Timișoara, Departementul de Chimie, 1994.

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Chu, Chung K., and David C. Baker, eds. Nucleosides and Nucleotides as Antitumor and Antiviral Agents. Boston, MA: Springer US, 1993. http://dx.doi.org/10.1007/978-1-4615-2824-1.

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Book chapters on the topic "Antitumor"

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Paz Lopes, Miriam Teresa, Dalton Dittz Júnior, and Fernanda de Oliveira Lemos. "Antitumor Phenylpropanoids." In Bioactive Essential Oils and Cancer, 215–30. Cham: Springer International Publishing, 2015. http://dx.doi.org/10.1007/978-3-319-19144-7_10.

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Fernandes, Janaina. "Antitumor Monoterpenes." In Bioactive Essential Oils and Cancer, 175–200. Cham: Springer International Publishing, 2015. http://dx.doi.org/10.1007/978-3-319-19144-7_8.

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Ribó, Marc, Antoni Benito, and Maria Vilanova. "Antitumor Ribonucleases." In Nucleic Acids and Molecular Biology, 55–88. Berlin, Heidelberg: Springer Berlin Heidelberg, 2011. http://dx.doi.org/10.1007/978-3-642-21078-5_3.

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Komiyama, Kanki, and Shinji Funayama. "Antitumor Agents." In The Search for Bioactive Compounds from Microorganisms, 79–103. New York, NY: Springer New York, 1992. http://dx.doi.org/10.1007/978-1-4612-4412-7_5.

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Kéri, Gy, I. Mezõ, A. Horváth, Zs Vadász, T. Bajor, M. Idei, T. Vántus, et al. "Novel antitumor peptide hormones with selective antitumor activity." In Peptides, 410–11. Dordrecht: Springer Netherlands, 1994. http://dx.doi.org/10.1007/978-94-011-0683-2_134.

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Magalhães, Hemerson Iury Ferreira, and Élida Batista Vieira de Sousa. "Antitumor Essential Oils." In Bioactive Essential Oils and Cancer, 135–74. Cham: Springer International Publishing, 2015. http://dx.doi.org/10.1007/978-3-319-19144-7_7.

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Lynch, Garrett R., and Montague Lane. "Other Antitumor Antibiotics." In Cancer Management in Man, 134–46. Dordrecht: Springer Netherlands, 1989. http://dx.doi.org/10.1007/978-94-009-1095-9_12.

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Zeng, Qing-Ping. "ART for Antitumor." In SpringerBriefs in Molecular Science, 29–39. Berlin, Heidelberg: Springer Berlin Heidelberg, 2015. http://dx.doi.org/10.1007/978-3-662-47688-8_3.

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Pagani, Mauro. "Antitumor/Cytostatic Drugs." In Cutaneous Drug Hypersensitivity, 297–304. Cham: Springer International Publishing, 2022. http://dx.doi.org/10.1007/978-3-030-82743-4_35.

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Marquez, Victor E. "Brain Antitumor Agents." In The Ups and Downs in Drug Design, 11–16. Boca Raton: CRC Press, 2021. http://dx.doi.org/10.1201/9781003203506-3.

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Conference papers on the topic "Antitumor"

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Ruzanova, V. S. "THE PERSONALIZED TECHNOLOGY OF CANCER TREATMENT "KARANAHAN" HAS THREE VECTORS OF THERAPEUTIC EFFECT." In I International Congress “The Latest Achievements of Medicine, Healthcare, and Health-Saving Technologies”. Kemerovo State University, 2023. http://dx.doi.org/10.21603/-i-ic-117.

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The aim of this work was to test the technology of treatment of malignant tumors "Karanahan" on the Lewis lung carcinoma model and to prove the existence of the third antitumor therapeutic vector of this technology – activation of antitumor immunity.
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Tikhonov, Sergey, Nataliya Tikhonova, N. V. Merzlyakova, and A. S. Ozhgihina. "PEPTIDES AS A FUNCTIONAL INGREDIENT FOR PREVENTIVE PRODUCTS." In I International Congress “The Latest Achievements of Medicine, Healthcare, and Health-Saving Technologies”. Kemerovo State University, 2023. http://dx.doi.org/10.21603/-i-ic-133.

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Clinical studies indicate that products from cow colostrum are well tolerated by the human body, non-toxic and safe for consumption. The aim of this study is to study the antitumor properties of isolated individual peptides from corvine colostrum on the cell line of rat glioblastoma C6. The study revealed that peptide R1 has antitumor activity, therefore it can be used as a functional ingredient in food products.
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Orel, V. E., O. Yu Rykhalskyi, A. D. Shevchenko, L. A. Syvak, N. O. Bezdenezhnykh, V. B. Orel, and A. V. Romanov. "Magnetic Memory in Antitumor Nanotherapeutics." In 2019 IEEE 39th International Conference on Electronics and Nanotechnology (ELNANO). IEEE, 2019. http://dx.doi.org/10.1109/elnano.2019.8783618.

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POZDNYAKOVA, Olga G., Galina A. BELAVINA, Alexander N. AVSTRIEVSKIKH, Andrey A. VEKOVTSEV, and Valery M. POZNYAKOVSKY. "Antioxidant Phytocomplex with Antitumor Activity." In XVIII International Scientific and Practical Conference "Modern Trends in Agricultural Production in the World Economy". Sibac, 2020. http://dx.doi.org/10.32743/kuz.agri.2020.1-11.

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Andreoni, Alessandra, Alberto Colasanti, Annamaria Kisslinger, Vincenzo Malatesta, Michele Mastrocinque, and Giuseppe Roberti. "Antitumor drugs as photochemotherapeutic agents." In Berlin - DL tentative, edited by Lars O. Svaasand. SPIE, 1991. http://dx.doi.org/10.1117/12.48198.

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Petrović, Biljana. "TRANSITION METAL ION COMPLEXES AS POTENTIAL ANTITUMOR AGENTS." In 1st INTERNATIONAL Conference on Chemo and BioInformatics. Institute for Information Technologies, University of Kragujevac,, 2021. http://dx.doi.org/10.46793/iccbi21.009p.

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Discovery of the antitumor activity of platinum complex, cisplatin, cis-Pt(NH3)2Cl2, and later carboplatin and oxaliplatin, led to the intensive investigation of the potential antitumor activity of the huge number of platinum complexes. Furthermore, it is well-known that platinum complexes express toxicity, numerous side effects and resistance, so the scientists make a lot of efforts to synthetize, beside Pt(II) and Pt(IV), other non-platinum compounds with potential antitumor activity, such as Pd(II), Ru(II/III) and Au(III) complexes. The goal of this study is to summarize the results of the investigation of the interactions between some mononuclear, homo- and hetero-polynuclear Pt(II), Pd(II), Ru(II/III) and Au(III) complexes with different sulfur- and nitrogen-donor biologically relevant nucleophiles. Among mononuclear complexes, the compounds with aromatic terpy (tepyridine) or bpma (bis-(2- pyridylmethyl)amine) and aliphatic dien (diethylentriamine) nitrogen-containing inert ligands were studied. Different homo- and hetero-polynuclear complexes with pz (pyrazine) or 4,4’-bipy (4,4’- bipyridine) as bridging and mostly en (ethylenediamine), bipy (2,2’-bipyridine) and dach (trans-1,2- diaminocyclohexane) as inert ligands were studied as well. The research was focused on the connection between the structure and the mechanisms of interactions with different biomolecules, such as L- cysteine (L-Cys), L-methionine (L-Met), tripeptide glutathione (GSH), guanosine-5’-monophosphate (5’-GMP), DNA and bovine serum albumin (BSA). Some of these complexes were selected for in vitro studies of the cytotoxicity on different tumor cell lines. Observed results contribute a lot as a guidance for the future design and determination of the structure-activity relationship (SAR) of different transition metal ion complexes.
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Milani, Valeria, Veit Buecklein, and Rolf Dieter Issels. "Abstract B11: Hyperthermia and antitumor immunity." In Abstracts: AACR International Conference on Translational Cancer Medicine--; Mar 21–24, 2010; Amsterdam, The Netherlands. American Association for Cancer Research, 2010. http://dx.doi.org/10.1158/1078-0432.tcme10-b11.

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Deryagina, Valentina Petrovna, Natalia Ilyinichna Ryzhova, Lyudmila Savluchinskaya, Leila Vladimirovna Krivosheeva, and Kirill Kirsanov. "ANTITUMOR EFFECT OF NITRIC OXIDE (NO) DONORS AND MECHANISMS OF ITS IMPLEMENTATION." In NEW TECHNOLOGIES IN MEDICINE, BIOLOGY, PHARMACOLOGY AND ECOLOGY. Institute of information technology, 2021. http://dx.doi.org/10.47501/978-5-6044060-1-4.23.

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The review discusses literature data and the results of our own studies on the role of nitric oxide in carcinogenesis. The antitumor potential of classical NO donors as cytotoxic compounds and modulators of signaling oncogenic pathways is analyzed.
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Alcolea, Marla, Renata Moraes Brito, Mahmi Fujimori, Adenilda Cristina Honorio-França, Eduardo Luzia França, and Paula Becker Pertuzatti. "IMMUNOMODULATORY EFFECTS OF HONEY FROM STINGLESS BEES AND HONEY BEES ON BREAST CANCER CELLS." In Brazilian Breast Cancer Symposium 2022. Mastology, 2022. http://dx.doi.org/10.29289/259453942022v32s2002.

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Objective: The limitations of current cancer treatments and their side effects have led to a growing interest in the study of natural compounds and alternative therapies such as apitherapy. Honey has in its constitution several substances that contribute to neutralize free radicals, such as phenolic compounds of which stand out in flavonoids and phenolic acids, besides having important antimicrobial and antitumor activities. However, the mechanisms of the antitumor action of honey and how the characteristics of honey of different species influence this mechanism are poorly understood. The aim of this study was to verify the antitumor action of honey bees (Apis mellifera) and stingless bees (Tetragonisca angustula) honey in mammary adenocarcinoma cell lines (MCF-7). Methods: Cell viability analyses were performed using fluorescence and flow cytometry methods, and oxidative balance through the release of superoxide anion (O2 − ) and production of the enzyme superoxide dismutase (SOD) in human peripheral blood mononuclear (MN) cells, MCF-7, and coculture of both. Results: Viability analyses in MN cells showed that honey samples, at concentrations of 100 mg/mL, 100 ng/mL, and 100 pg/mL, do not present cytotoxicity to cells. But in MCF-7 cells, there was a decrease in viability with stingless bee honey (100 mg/mL), showing the highest cytotoxic action and reducing the viability of cancer cells by 30.4%. The same honey sample caused an immunomodulatory effect on both MN and cancer cells, stimulating greater release of O2 − and SOD enzyme activity in these cells. While in the coculture, there was a greater release of O2 − and a decrease in enzymatic activity. Conclusion: The results showed that especially stingless bee honey acts on the oxidative stress of cells, and this might be the mechanism related to its antitumor action. Thus, honey can play a potential role as a preventive agent and complementary therapy against breast cancer.
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Franich, Andjela, Ivana Vasić, Snežana Rajković, Aleksandar Arsenijević, Marija Milovanović, Nebojša Arsenijević, Jelena Milovanović, and Marija Živković. "CYTOTOXICITY OF CATIONIC DINUCLEAR PLATINUM(II) COMPLEXES IN AN EXPERIMENTAL MODEL OF MOUSE COLON CANCER." In 1st INTERNATIONAL Conference on Chemo and BioInformatics. Institute for Information Technologies, University of Kragujevac, 2021. http://dx.doi.org/10.46793/iccbi21.293f.

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The series of nine dinuclear platinum(II) complexes, [{Pt(L)Cl}2(μ-X)]2+ (where L is two NH3 or bidentantly coordinated diamine ligand – ethylenediamine, en; (±)-1,2-propylenediamine, 1,2-pn; isobutylenediamine, ibn; trans-(±)-1,2-diaminocyclohexane, dach; 1,3-propylenediamine, 1,3-pd; 2,2- dimethyl-1,3-propylenediamine, 2,2-diMe-1,3-pd; (±)-1,3-pentanediamine,1,3-pnd, and X is a bridging pyrazine (pz) or pyridazine (pydz) ligand) have been synthesized and characterized. The antitumor potential of these complexes against CT26 cells were determined by in vitro and in vivo assays. A murine model of heterotopic colon cancer tumor was induced in immunocompetent BALB/c mice for investigating antitumor potential of the Pt(II) complexes in vivo. It was found that complexes Pt1, Pt2 and Pt7 shows significant in vitro cytotoxic activity against mouse colon carcinoma CT26 cells, while all these complexes show moderate apoptotic effect. Complexes Pt1 and Pt7 arrested CT26 cells in G2/M phase of cell cycle, while complexes Pt5 and Pt6 exerted the highest antiproliferative effect which was evaluated by detection of Ki67 expressing cells. Complexes Pt1 and Pt2 performed significant in vivo antitumor effects reducing the growth of primary tumor and the incidence of lung and liver metastases without causing the significant hepato- and nephro- toxicity.
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Reports on the topic "Antitumor"

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Conejo-Garcia, Jose R. Reprogramming Antitumor Immune Responses with microRNAs. Fort Belvoir, VA: Defense Technical Information Center, October 2012. http://dx.doi.org/10.21236/ada585107.

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Conejo-Garcia, Jose R. Reprogramming Antitumor Immune Responses with microRNAs. Fort Belvoir, VA: Defense Technical Information Center, October 2013. http://dx.doi.org/10.21236/ada595676.

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Rayhim, Rayhana, and Jeannie S. Strobl. Augmentation of the Differentiation Response to Antitumor Antimalarials. Fort Belvoir, VA: Defense Technical Information Center, July 2004. http://dx.doi.org/10.21236/ada432050.

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Hill, Ann. Vaccine Vector for Sustained High-Level Antitumor CTL Response. Fort Belvoir, VA: Defense Technical Information Center, January 2011. http://dx.doi.org/10.21236/ada546083.

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Wang, He, Jun Chen, Xiaoling Wang, and Jun Dang. Neoadjuvant immune checkpoint inhibitor in combination with chemotherapy or chemoradiotherapy in resectable esophageal cancer: A systematic review and meta-analysis. INPLASY - International Platform of Registered Systematic Review and Meta-analysis Protocols, June 2022. http://dx.doi.org/10.37766/inplasy2022.6.0052.

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Review question / Objective: It remains unclear whether addition of immune checkpoint inhibitor (ICI) to neoadjuvant chemoradiotherapy (nCRT) or neoadjuvant chemotherapy (nCT) can increase antitumor efficacy in resectable esophageal cancer (EC). we performed the systematic review and meta-analysis to assess antitumor efficacy and safety of nICRT and nICT, and made a comparison with nCRT and nICT. We used pathological complete response (pCR) as the primary outcomes of interest. Condition being studied: Initial findings from a number of phase 1 or 2 trials have supported the tolerability and/or antitumor efficacy of ICI plus nICRT (nICRT) and nICT (nICT). However, the superiority of this combination strategy remains uncertain due to lack of randomized control trials (RCTs) with long-term outcomes. Moreover, there are still outstanding questions such as the selection of nICRT or nICT, the ideal predictive biomarkers, and timing of surgical resection.
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Fenton, Bruce M. Potentiation of Prostate Cancer Radiotherapy Using Antiangiogenic and Antitumor Therapies. Fort Belvoir, VA: Defense Technical Information Center, October 2007. http://dx.doi.org/10.21236/ada478113.

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Li, Chun. Radiation-Induced Chemosensitization: Potentiation of Antitumor Activity of Polymer-Drug Conjugates. Fort Belvoir, VA: Defense Technical Information Center, April 2002. http://dx.doi.org/10.21236/ada406209.

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Fenton, Bruce M. Potentiation of Prostate Cancer Radiotherapy Using Combined Antiangiogenic and Antitumor Therapies. Fort Belvoir, VA: Defense Technical Information Center, October 2005. http://dx.doi.org/10.21236/ada446439.

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Li, Chun. Radiation Induced Chemosensitization: Potentiation of Antitumor Activity of Polymer-Drug Conjugates. Fort Belvoir, VA: Defense Technical Information Center, April 2003. http://dx.doi.org/10.21236/ada415707.

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Basu, Sayani. Monoclonal Antibody Therapy: A New Hope in Cancer Treatment. Natur Library, November 2020. http://dx.doi.org/10.47496/nl.blog.14.

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The remarkable specificity, high efficacy and the ability to elicit an antitumor response indicate that monoclonal antibody therapy offers promise in the treatment of malignancy and appears to be clinically relevant
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