Dissertations / Theses: 'Antineoplastika'

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Wan, Jung Wing. "Novel ether lipids as antineoplastic agents." Thesis, University of Southampton, 1997. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.242627.

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Danica, Jović. "Sinteza, karakterizacija i biološka ispitivanja fulerenol/doksorubicin nanokompozita." Phd thesis, Univerzitet u Novom Sadu, Prirodno-matematički fakultet u Novom Sadu, 2018. https://www.cris.uns.ac.rs/record.jsf?recordId=106903&source=NDLTD&language=en.

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U radu je predstavljena sinteza i karakterizacija novog fulerenol/doksorubicin nanokompozita, sintetisanog sa ciljem dobijanja potencijalne nove nanoformulacije postojećeg antineoplastika doksorubicina, koja bi pokazala veću biološku aktivnost uz smanjenje neželjenih sporednih efekata koje sam lek izaziva, na prvom mestu kardiotoksičnosti.Nanokompozit fulerenol/doksorbicin je okarakterisan brojnim metodama prateći dva osnovna eksperimentalna pristupa: molekulsko-spektroskopske metode (XPS, denzitometrija i transportne osobine, NMR, UPLC, Ramanska i UV-spektroskopija, SFM) i metode nanokarakterizacije (DLS, AFM, TEM), kao i računske simulacije(RDF). Osnovni cilj ispitivanja je bila detekcija postojanja nekovalentnog nanokompozita koji ostvaruju doksorubicin i fulerenolske nanočestice u vodenom rastvoru. Rezultati karakterizacije jasno i nedvosmisleno ukazuju na postojanje nekovalentnih interakcija unutar nanokompozita, što dalje utiče na organizaciju i udruživanje čestica, a što uslovljava i drugačiju biološku aktivnost takvog sistema u odnosu na pojedinačne komponente. Rezultati bioloških ispitivanja na in vitro modelu različitih tumorskih ćelijskih linija pokazuju značajan antiproliferativni efekat nanokompozita, kao i selektivnost prema tumorskim u odnosu na zdravu ćelijsku liniju. Eksperimenti na in vivo modelu zebrica potvrđuju smanjenje toksičnosti nanokompozita u poređenju sa lekom, primarno kardiotoksičnosti. Računske simulacije, mikroskopski i spektroskopski podaci, kao i rezultati in vitro i in vivo studija ukazuju na to da nekovalentne interakcije između fulerenola i doksorubicina mogu biti ključni korak u stvaranju sinergističkog sistema za dostavu leka u biološki sistem.Multipotentnost fulerenola kao nanonosača lekova i nespecifičnost strukture doksorubicina kao leka, ukazuje na to da bi fulerenol mogao biti efikasan nanonosač i drugih antineoplastika, što daje prostora za unapređenje antitumorskih osobina lekova posredstvom istovremene administracije leka.
The focus of this thesis was the synthesis and characterization of a novel fullerenol/doxorubicin nanocomposite, with the aim to obtain a potential nanoformulation of antineoplastic drug doxorubicin, which would express greater biological activity and lower level of adverse effects than the drug itself, in the first place cardiotoxicity.Nanocomposite fullerenol/doxorubicin was characterized by means of numerous methods following two main experimental approaches: molecular-spectroscopic methods (XPS, densitometry and transport properties, NMR, UPLC, Raman and UVspectroscopy, SFM) and mehods of anocharacterisation (DLS, AFM, TEM), as well as computer simulations (RDF). The goal of characterization was detection of non-covalent interactions within nanocomposite that are established between fullerenol nanoparticles and doxorubicin in aqueous solution. The results clearly indicate the existence of non- covalent interactions within nanocomposite that affect the organization and assembling of the particles, which further exhibit different biological activity of such a system in comparison to components themselves. Results of biological activity on in vitro model of different tumor cell lines show significant antiproliferative effect of nanocomposite, as well as selectivity towards tumor cell lines. Experiments conducted on in vivo zebrafish model confirm the lowering ofthe adverse effects of the drug, especially cardiotoxicity, in case when nanocomposite was applied. Computer simulations, microscopic and spectroscopic results combined with encouraging in vitro and in vivo results point out that non-covalent interactions between fullerenol nanoparticles and doxorubicin may present the keyrole in formation of a synergistic system for nanodrug delivery into biological system. Multipotential of fullerenol nanoparticles as a nanocarrier and non-specific structure of doxorubicin as a drug imply that fullerenol may serve as a efficient nanocarrier of numerous other antineoplastics, which further allows the improvement of antitumor properties of drugs withsimultaneous drug administration.

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Conesa, Milián Laura. "Synthesis of combretastatin analogues with antineoplastic properties." Doctoral thesis, Universitat Jaume I, 2019. http://hdl.handle.net/10803/667097.

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This doctoral thesis belongs to the field of medicinal and pharmacological chemistry. Its aim is the synthesis, characterization and biological evaluation of three families of aminocombretastatin derivatives, compound with antimitotic and antiangiogenic properties. The first group contains a carbamate function in its structure. These derivatives have been studied as antimitotic and vascular disrupting agents. The second family has been designed from sorafenib drug, with the aim of studying its antiangiogenic effects. Regarding the third family, these have been designed as multitarget compounds, with both antiangiogenic and immunomodulatory properties. Finally, in vivo studies have been developed with the aim of knowing all the perspectives of a biological evaluation process. In conclusion, several compounds have been obtained from the same general structure, able to interact with different targets involved in cancer disease, thus improving the effect offered by aminocombretastatin.
Esta tesis doctoral se enmarca en el campo de la química médica y farmacológica. Tiene como objetivo la síntesis, caracterización y evaluación biológica de tres familias de derivados de aminocombretastatina, compuesto con propiedades antimitóticas y antiangiogénicas. El primer grupo contiene una función carbamato en su estructura. Estos se han estudiado como agentes antimitóticos y disruptores de la vasculatura. La segunda familia se ha diseñado a partir del fármaco sorafenib, con el objetivo de estudiar sus efectos antiangiogénicos. Respecto a la tercera familia, se trata de compuestos multidiana, con propiedades antiangiogénicas e inmunomoduladoras. Finalmente, se han desarrollado estudios in vivo con el objetivo de conocer todas las perspectivas de un proceso de evaluación biológica. Como conclusión, destacar que a partir de una misma estructura general se han obtenido varios compuestos que interactúan con diferentes dianas involucradas en la enfermedad del cáncer, mejorando así pues el efecto ofrecido por la aminocombretastatina.

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Molyneux, Gemma. "Studies on the haemotoxicity of antineoplastic agents." Thesis, University College London (University of London), 2006. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.435080.

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Hedmer, Maria. "Monitoring of occupational exposure to antineoplastic drugs." Malmö : Lund University, 2006. http://theses.lub.lu.se/scripta-archive/2006/04/18/med_1298/Maria_H_kappa.pdf.

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Chen, Alina. "New polyamine analogues as potential antineoplastic agents." Scholarly Commons, 2000. https://scholarlycommons.pacific.edu/uop_etds/2680.

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The naturally occurring polyamines play an essential role in cell growth and proliferation. The levels of polyamines have been shown to increase in rapidly proliferating cancer cells. Therefore, compounds that inhibit enzymes in polyamine biosynthetic pathway may have therapeutic potential. Compounds capable of providing both in vitro and in vivo inhibition of almost all enzymes in the polyamine biosynthetic pathway are known. An exception is the lack of an agent that inhibits spermidine/spermine N 1 -acetyltransferase (SSAT), the rate-limiting enzyme in the catabolism of polyamines. The design, synthesis and characterization of five new polyamine analogues as potential inhibitors of SSAT are presented. Three compounds, N 1 -[3-(propenamido) propyl]-1,4-diaminobutane dihydrochloride 5 , N 1 -[3-(maleimido)propyl]-1,4-diamino-butane dihydrochloride 7 and N 1 -[3-(2-bromoacetamido)propyl]-1,4-diaminobutane dihydrochloride 9 , were designed as active-site-directed affinity label inhibitors. Two compounds, N-[N-(5-acetamido-2-hydroxypentyl-3-aminopropyl)]-1,4-diaminobutane trihydrochloride 12 and N-[3-(2-hydroxyethylamino)propyl]-1,4-diaminobutane trihydrochloride 14 , were designed as transition state-like analogue inhibitors. These compounds were synthesized using one key intermediate, N-(3-aminopropyl)-N,N ′ -bis-(tert-butoxycarbonyl)-1,4-diaminobutane 3 . Three of these synthesized compounds, 5 , 7 and 12 were evaluated for their ability to inhibit SSAT. The enzyme used was a crude extract of human large cell undifferentiated lung carcinoma cell line NCI H157 cells. These synthetic analogues when tested against the crude enzyme extract at concentrations of 0.05, 0.1, 1 and 5 μM appeared to show no effects on the activity of SSAT.

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Bossaer, John B. "Addressing Potential Interactions Between Antineoplastics and Dietary Supplements." Digital Commons @ East Tennessee State University, 2015. https://doi.org/10.2146/ajhp140295.

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Rey, Allan W. "Synthetic studies directed towards the antineoplastic macrolide bryostatins." Thesis, University of Ottawa (Canada), 1990. http://hdl.handle.net/10393/5938.

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This thesis describes stereocontrolled and practical routes to the C(1)-C(9), C(17)-C(20), and C(21)-C(27) synthons of bryostatins, which are a closely related family of 20-membered ring lactones embedding 1,3-polyol units. Bryostatins are isolated in minute quantities from the marine Bryozoan Bugula neritina and possess exceptional antineoplastic activity. Membrane-enclosed enantioselective enzymatic hydrolysis was successfully employed for the generation of gram quantities of the versatile building block (3R)-methoxymethoxypentadioic acid, monomethyl ester (51) (Chapter 2). This compound was used in the synthesis of the C(1)-C(5) segment of bryostatins. Preliminary synthetic studies towards the C(1)-C(9) subunit are described in Chapter 3. Wittig and dithiane approaches were unfortunately unsuccessful for the connection of an enzymatically derived 5 carbon unit with a D-pantolactone derived 4 carbon unit. Chapter 4 describes the practical synthesis of the C(1)-C(9) fragment of bryostatin in forms suitable for both structure/activity studies and synthetic elaboration. The pivotal step utilized a diastereoselective Mukaiyama aldol condensation of a diketene derived silylenol ether with an enzymatically derived chiral $\beta$-alkoxyaldehyde. Chapter 5 details the conversion of D-pantolactone and of D-galactono-1,4-lactone into the C(17)-C(20) and C(21)-C(27) synthons of bryostatins via a chiron approach. A study of nucleophilic additions onto chiral substituted $\gamma$-lactol templates is discussed in Chapter 6. This provided valuable information regarding the coupling of the C(17)-C(20) and C(21)-C(27) segments of bryostatins. As well, the results demonstrate the potential utility of $\gamma$-lactols as templates--a relatively unexplored area in asymmetric synthetic chemistry.

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Parker-, Johnson Kitani A. "An evaluation of novel antineoplastic agent on prostate cancer." DigitalCommons@Robert W. Woodruff Library, Atlanta University Center, 2003. http://digitalcommons.auctr.edu/dissertations/3074.

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This study examines the effects of novel antineoplastic agents(isochalcones) on human metastatic prostate cancer cell lines by screening cells for their relative antiproliferative effects, measuring the protein expression levels of specific oncogenes by Western blotting, and evaluating an array of genes ( 5184) to determine possible mechanisms of action of these novel isochalcones. The array data were supported by real-time polymerase chain reaction (PCR) techniques. The antineoplastic agents were screened in human metastatic prostate cancer cell lines (LNCaP, DU145, PC-3, and MDA-PCa-2b) and non-cancerous prostate epithelial cell line PZ-HPV-7 in concentrations ranging from nanomolar to millimolar. The alamar blue exclusion dye assay, a redox indicator, was used to evaluate cell proliferation when compared to the untreated control. DJ52 demonstrated a growth inhibitory effect on LNCaP, PC-3, and DU145 cell lines at the micromolar concentration (p<0.05). Based on these data, 1 x 106 cells were treated, protein isolated, and expression levels of epidermal growth factor (EGF) and omithine decarboxylase (ODC) were measured and compared to theuntreated controls. These data indicated a dose-dependent decrease of expression of EGF and ODC, therefore, suggesting that other key oncogenes may also have a decrease in expression when treated with these novel antineoplastic agents. Therefore, gene arrays were used to identify possible families of genes and/or specific pathways that may be responsible for the antiproliferative effects noted. It was determined that the key families of genes significantly induced by these agents (Pathways 4®) were proapoptotic and cell cycle regulators. ABI 7700 Prism was used to perform quantitative RT-PCR via the AB Sequence Detector® software.

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Arshad, Usman [Verfasser]. "Population pharmacokinetic modeling to understand antineoplastic treatment / Usman Arshad." Bonn : Universitäts- und Landesbibliothek Bonn, 2020. http://d-nb.info/1239730233/34.

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Madiga, Maphuti Carol. "Antioxidative, anti-inflammatory and antineoplastic potential of dicerocaryum species." Thesis, University of Limpopo (Turfloop Campus), 2007. http://hdl.handle.net/10386/926.

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Rillo, Ryan A. "Health Issues Related to the Management of Antineoplastic Drugs." University of Toledo Health Science Campus / OhioLINK, 2009. http://rave.ohiolink.edu/etdc/view?acc_num=mco1243889530.

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Horgan, Carmel M. T. "Studies on Mitozolomide (CCRG 81010), a new antineoplastic agent." Thesis, Aston University, 1985. http://publications.aston.ac.uk/12474/.

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Bossaer, John B., and Christan M. Thomas. "Drug Interaction Database Sensitivity With Oral Antineoplastics: An Exploratory Analysis." Digital Commons @ East Tennessee State University, 2017. https://dc.etsu.edu/etsu-works/2328.

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Purpose: Drug interactions are a concern in oncology with the shift toward oral antineoplastics (OAs). Using electronic databases to screen for drug interactions with OAs is a common practice. There is little literature to guide clinicians on the reliability of these systems with OAs. The primary objective of this study was to explore the sensitivity of commonly available drug interaction databases in detecting drug interactions with OAs. Methods: A list of 20 drug interactions with OAs was developed by two Board-certified oncology pharmacists. The list included multiple types of drug interactions. The sensitivity in detecting these interactions by MicroMedex, Facts & Comparisons, Lexi-Interact, and Epocrates were evaluated. These databases were chosen based on their local availability and widespread use in practice. Drugs.com was evaluated as a surrogate for a patient-accessible drug interaction database. The Cochran Q test was used to assess the sensitivity distribution across the five groups. Results: Lexi-Interact and Drugs.com had a sensitivity of 95% for the 20 tested drug interaction pairs. Epocrates had a sensitivity of 90%, and both Micromedex and Facts & Comparisons had a sensitivity of 70%. There was a statistically significant difference (P = .016) in the distribution across the databases in detecting clinically significant drug interactions. Conclusion: Commonly used databases for identifying drug interactions with oral antineoplastics vary significantly in their sensitivity. Clinicians should not rely on a single database and should consider using multiple resources as well as sound clinical judgment. Further work is needed in this area.

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Bossaer, John B., and Christian Thomas. "Drug Interaction Database Sensitivity with Oral Antineoplastics: An Exploratory Analysis." Digital Commons @ East Tennessee State University, 2016. https://dc.etsu.edu/etsu-works/2339.

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Kanyanda, Stonard Sofiel Elisa. "Screening of natural products and Alkylating agents for Antineoplastic Activity." Thesis, University of the Western Cape, 2007. http://etd.uwc.ac.za/index.php?module=etd&action=viewtitle&id=gen8Srv25Nme4_6433_1363357514.

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Background and objectives: Apoptosis is a process in which a cell programmes its own death. It is a highly organized physiological mechanism in which injured or damaged cells are destroyed. Apart from physiological stimuli however, exogenous factors can induce apoptosis. Many anti-cancer drugs work by activating apoptosis in cancer cells. Natural substances have been found to have the ability to induce apoptosis in various tumour cells and these substances have been used as templates for the construction of
novel lead compounds in anticancer treatment. On the other hand, alkylating agents such as cisplatin, cis- [PtCl2 (NH3) 2] have been widely used as antineoplastic agents for a
wide variety of cancers including testicular, ovarian, neck and head cancers, amongst others. However, the use of cisplatin as an anticancer agent is limited due to toxicity and resistance problems. The aim of this present study was to screen the leaves of Rhus laevigata, a South African indigenous plant, for the presence of pro-apoptotic and
anti-proliferative natural compounds and also to screen newly synthesised palladium based complexes (15 and 57) and a platinum based complex (58) for their antineoplastic
activities tested against a panel of cell lines. Results. The results showed that crude methanol extracts from Rhus laevigata as well as the newly synthesised palladium based complexes (15 and 57) and a platinum based complex (58) induced apoptosis in the cell lines tested, as demonstrated by the externalization of phosphatidylserine, mitochondrial membrane permeabilization,caspase-3 activation, and DNA fragmentation. Caski (cervical cancer) and H157 (non small cell lung carcinoma) cell lines treated with the methanol extract from Rhus laevigata however, were more resistant to apoptosis induction. Among the metallocomplexes, complexes 15 and 57, palladium based complexes, were the most active. Conclusion: The methanol extract from the leaves of Rhus laevigata contain pro-apoptotic and antiproliferative natural compound(s), which need to be characterised and elucidated as they could provide the much-needed lead compounds in the fight against cancer. On the other hand the newly synthesized palladium complexes also need further evaluation to
see if they can be used as anticancer agents that can overcome the problems associated with cisplatin.

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Payne, Jason N. "Development of Dihydrochalcone Functionalized Gold Nanoparticles for Augmented Antineoplastic Activity." TopSCHOLAR®, 2016. http://digitalcommons.wku.edu/theses/1749.

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Phloridzin, an antidiabetic and antineoplastic agent usually found in fruit trees, is a dihydrochalcone constituent that has a clinical/pharmaceutical significance as a sodiumglucose linked transport 2 (SGLT2) inhibitor. Phloridzin never experienced widespread clinical usage in the pharmaceutical market due to its side effects and poor bioavailability when compared to other antidiabetic therapeutics. The poor bioavailability is primarily attributed to the degradation of the glycosidic bond of the phloridzin, resulting in the formation of phloretin, the aglycone of phloridzin and glucose. While phloretin displays a reduced capacity of SGLT2 inhibition, this nutraceutical shows enhanced antineoplastic activity in comparison to phloridzin. Gold nanoparticles (AuNPs) have been explored in improving the bioavailability of many drugs and therefore we opt for gold nanoparticle mediated delivery of phloridzin and phloretin and exploration of their anticancer mechanism. In this study, we have synthesized phloridzin and phloretin conjugated gold nanoparticles (Phl-AuNP and Pht-AuNP) in a single-step, rapid, biofriendly processes. The synthesized AuNPs morphology and elemental composition was characterized via transmission electron microscopy, UV-Vis spectroscopy, scanning electron microscopyenergy dispersive x-ray spectroscopy, and thermogravimetric analysis. Assessment of the antineoplastic potency of the dihydrochalcone-conjugated AuNPs against cancerous cell lines was accomplished through monitoring via flow cytometry. We posit that the functionalization of these chalcones onto the gold nanoparticles’ surface has improved the pharmacokinetic profile of phloridzin and phloretin.

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Furbacher, Todd Raymond. "Bioassay-guided isolation of potential antineoplastic natural products from Southwestern plants." Diss., The University of Arizona, 2001. http://hdl.handle.net/10150/279927.

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This dissertation details the investigation of numerous plants for potential antineoplastic compounds. 144 plants (391 extracts) were prescreened with an assortment of assays. The pre-screens included an Agrobacterium tumefaciens/potato disk gall tumor inhibition assay, a Saccharomyces cerevisiae mutant topoisomerase assay, and an Escherichia coli plasmid scission assay. Bioassay-guided fractionation was conducted on three plants, Phoradendron juniperinum, Psorothamnus thompsoniae , and Acourtia thurberi, using a different assay for each. Phoradendron juniperinum (Viscaceae) was screened with a plasmid scission assay and the novel compound, 5-caffeoyl-epi-quinic acid (I) was isolated, the first chlorogenic acid to be reported for the genus. Chemical structure was established using NMR and MS data and published structural information. The EC₅₀ for 5-caffeoyl- epi-quinic acid-mediated plasmid DNA cleavage was 76 μM. Fractionation of Psorothamnus thompsoniae (Fabaceae) was directed using the potato disk assay. The active component was dalrubone (II). P. emoryi was fractionated to obtain dalrubone and to search for related compounds. 5-Methoxydalrubone (III) was isolated and tested with dalrubone in cell line assays. 5-Methoxydalrubone was active against MCF-7 (IC₅₀ = 28.2 μM), while dalrubone (IC₅₀ = 1.3 mM) was not. Neither compound significantly inhibited the growth of NCI-H460 or SF-268. Acourtia thurberi (Asteraceae) was active in the yeast mutant assay. Fractionation yielded the sesquiterpene, 14,15-diacetoxy-,8-hydroxy-,3-(3-methylbutanoyl)-14, 15-epoxy-isocedrene (IV). This compound was weakly active against the topoisomerase II sensitive yeast strain, RS321N, with an IC12 of 342 μg/mL. The isocedrene was active in the yeast assay but inactive against human topoisomerase IIalpha. Ten celastroloids (unsaturated, oxygenated D:A-friedo-nor-oleanane triterpenoids from Sri Lankan Celastraceae) and their derivatives, some of which were also weakly active against RS321N, were tested for activity against human topoisomerase IIalpha. Demethylzeylasterone (ex. Kokoona zeylanica) strongly inhibited topo IIalpha with an IC50 of 17.6 μM. All others, including the structurally similar zeylasterone, possessed no activity at 100 μM. Demethylzeylasterone was determined to be a "catalytic inhibitor," preventing DNA from binding to the enzyme while not interacting with the DNA itself. Demethylzeylasterone selectively inhibits the MCF-7 breast cancer cell line with an IC50 of 12.5 μM.

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Rivero-MuÌˆller, Adolfo. "Speciation and reactivity of the antineoplastic copper-based compound : casiopeina II." Thesis, University of Surrey, 1999. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.301319.

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Avebring, Johanna, and Anna-Karin Karlsson. "Att utsätta sig för risker i tjänsten : Sjuksköterskans hantering av antineoplastiska läkemedel – En litteraturstudie." Thesis, Karlstads universitet, Fakulteten för hälsa, natur- och teknikvetenskap (from 2013), 2019. http://urn.kb.se/resolve?urn=urn:nbn:se:kau:diva-72145.

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Introduktion: Under 1970-talet kom den yrkesmässiga exponeringen i samband med behandling med antineoplastiska läkemedel (ANL) i fokus. Exponeringen kan uppstå vid beredning, administrering, hantering av spill, avfall och utsöndring från patient. Vid långvarig exponering eller enstaka högdos exponeringar av dessa läkemedel finns en förhöjd risk för genetiska skador och/eller cancer. Syfte: Syftet med litteraturstudien var att belysa de orsaker som bidrar till att sjuksköterskan exponeras för ANL i tjänsten. Metod: Litteraturstudien genomfördes med utgångspunkt i Polit och Becks struktur för arbete med litteraturstudier i nio steg. Databaser som användes för litteratursökning var Cinahl och PubMed. Databearbetningen av materialet från litteratursökningen utfördes med en induktiv ansats. Resultat: Fem teman i materialet framträdde varefter resultaten bearbetades. Identifierade teman var arbetsmiljö & arbetskultur, riktlinjer & säkerhetsrutiner, utbildning & uppföljning, attityd & följsamhet samt kultur & kontext. Utifrån dessa undergrupper framträdde två huvudteman till varför sjuksköterskor exponeras för ANL i tjänsten: organisatoriska orsaker samt personliga orsaker. Slutsats: För en mer säker hantering av ANL för sjuksköterskor är det viktigt att det finns ett tydligt stöd från organisationen i form av riktlinjer, kontroller, uppföljning, utrustning och utbildning. En ökad kunskap ger en positiv påverkan på attityder till användning av personlig skyddsutrustning vid hantering.

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Salvetti, Raul. "Sintesi studio in vitro di nuovi analoghi nucleosidi a potenziale attivita' antivirale o antineoplastica." Montpellier 2, 2004. http://www.theses.fr/2004MON20018.

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La recherche de nouvelles structures nucléosidiques susceptibles d'interférer spécifiquement avec la multiplication des virus reste un défi à relever. Dans la première partie de ce travail, nous nous sommes attachés à la préparation de dérivés nucléosidiques en série 6-aminouracile. Aucun des dérivés synthétisés dans cette première partie n'a présenté d'activité antivirale notable contre un large spectre de virus (VIH, VHB, YFV, BVDV). Par la suite, le deuxième chapitre a été consacré à la synthèse et à l'étude de dérivés en série 5-halogéno-6-aminouridine comme inhibiteurs potentiels de la thymidine phosphorylase, enzyme qui est impliqué dans le phénomène d'angiogénèse. Dans la troisième partie, nous avons synthétisé des dérivés en série 6-(4-alkylanilino) uridines à visée antiherpétique comme inhibiteur potentiel de l'ADN-uracil Glycosylase du virus de l'herpès simplex 1. Enfin, dans la dernière partie de ce travail, la synthèse enzymatique de 2'-désoxynucléosides en utilisant des réactions de transglycosylation a été abordée.

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Ganley, Brian. "Investigations into the chemical mechanisms of biological activity by heterocyclic di-N-oxides and 1,2 benzodithiolan-3-one 1-oxides." free to MU campus, to others for purchase, 2000. http://wwwlib.umi.com/cr/mo/fullcit?p9999285.

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23

Arab, Sara. "Studies of the antineoplastic activity of verotoxin in vitro and in vivo." Thesis, National Library of Canada = Bibliothèque nationale du Canada, 1997. http://www.collectionscanada.ca/obj/s4/f2/dsk2/ftp02/NQ27869.pdf.

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Dymond, Marcus Karl. "An investigation into the mechanism of action of amphiphilies with antineoplastic properties." Thesis, University of Southampton, 2001. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.250080.

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Xie, Yanqi. "SEMISYNTHETIC AURONES: A FAMILY OF NEWLY DISCOVERED TUBULIN INHIBITORS AS ANTINEOPLASTIC AGENTS." UKnowledge, 2019. https://uknowledge.uky.edu/biochem_etds/44.

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Aurones belong to an uncommon class of plant flavonoids that provide the bright yellow coloration of some ornamental flowers and that possess a range of biological activities. Structure-activity relationships (SAR) in the aurone pharmacophore identified heterocyclic variants of the (Z)-2-benzylidene-6-hydroxybenzofuran-3(2H)-one scaffold that possessed low nanomolar in vitro potency in cell proliferation assays using various cancer cell lines, in vivo potency in prostate cancer PC-3 xenograft and zebrafish models, selectivity for the colchicine-binding site on tubulin, and absence of appreciable toxicity. Among the biologically active analogs developed in the course of this dissertation work were (Z)-2-((2-((1-ethyl-5-methoxy-1H-indol-3-yl)methylene)-3-oxo-2,3-dihydrobenzofuran-6-yl)oxy)acetonitrile (5a) and (Z)-6-((2,6-dichlorobenzyl)oxy)-2-(pyridin-4-ylmethylene)benzofuran-3(2H)-one (5r). These two aurones 5a and 5r inhibited in vitro PC-3 prostate cancer cell proliferation with IC50 values below 100 nM. A xenograft study in nude mice using 10 mg/kg of 5a for 18 days had no effect on mice weight, and aurone 5a did not inhibit, as desired, the human ether-à-go-go-related (hERG) potassium channel. Cell cycle arrest data, comparisons of the inhibition of cancer cell proliferation by aurones and known antineoplastic agents, and in vitro inhibition of tubulin polymerization indicated that aurone 5a disrupted tubulin dynamics. Based on a National Cancer Institute COMPARE analysis, studies using computer-based molecular docking and liquid chromatography-electrospray ionization-tandem mass spectrometry studies, aurone 5a targets the colchicine-binding site on tubulin. In addition to solid tumors, aurones 5a and 5r strongly inhibited in vitro a panel of human leukemia cancer cell lines and the in vivo myc-induced T cell acute lymphoblastic leukemia (T-ALL) in a zebrafish model. In summary, aurones possess a pharmacophore of considerable potential in the search for new antineoplastic agents for the clinical treatment of human cancers.

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26

Shishido, Stephanie Nicole. "Efficacy of gap junction enhancers and antineoplastic drugs in mammary carcinoma models." Diss., Kansas State University, 2013. http://hdl.handle.net/2097/16894.

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Doctor of Philosophy
Department of Diagnostic Medicine/Pathobiology
Thu Annelise Nguyen
Preclinical animal models of mammary carcinoma formation are vital for the advancement of cancer research, specifically in drug development. Two different types of animal models were utilized to determine the efficacy of combinational treatment of common antineoplastic drugs and the new class of primaquines that act as gap junction enhancers (PQs) at attenuating mammary tumor growth. The classic xenograft mouse model was used to show that PQs could increase the efficacy of cisplatin and paclitaxel. Combinational treatment induced an upregulation of connexin and caspase expression in the isolated tumor. Next the transgenic PyVT mouse model was characterized by multiple factors, including hormone receptor status, molecular markers for survival and proliferation, tissue histopathology, and secondary metastases during multiple stages of tumor development. This model showed limited therapeutic response to the antineoplastic drugs tested. PQ1 effectively attenuated tumor growth at all stages of tumorigenesis in the PyVT model, while PQ7 was determined to be an effective chemopreventive compound rather than chemotherapeutic. The PQs altered the expression profiles of connexins during tumorigenesis. Together the results indicate that PQs have an anticancer effect that is more efficient at attenuating tumor growth than the common antineoplastic compounds. Lastly the PyVT mouse model was used to determine the efficacy of antineoplastic compounds on male mammary carcinoma development. Interestingly, the antineoplastic compound that attenuated female mammary carcinoma growth did not produce a therapeutic response in the males and vice versa, suggesting a need for further studies into the male response to therapy.

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27

Ramirez, Daniel A. Kane Robert R. "Synthesis of protected amino thymidines and new thiol derivatives of the vascular targeting agent combretastatin A-4." Waco, Tex. : Baylor University, 2006. http://hdl.handle.net/2104/5008.

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28

Hon, Chun-Yip. "Healthcare workers and antineoplastic drugs : evaluating the risks and identifying determinants of exposure." Thesis, University of British Columbia, 2012. http://hdl.handle.net/2429/42505.

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Healthcare workers’ exposure to antineoplastic drugs may occur through handling of the drugs and/or via contact with drug-contaminated surfaces. However, studies have been limited to select departments and/or certain job titles. This may lead to an underestimate of the risk as the drugs circulate within a facility known as the hospital medication system (process flow of drugs). This study aimed to answer the following questions related to antineoplastic drugs and the hospital medication system: 1) is contamination found on surfaces located throughout, 2) are workers throughout occupationally exposed (dermal and urinary contamination), and 3) what factors are associated with surface contamination and occupational exposure? Site observations were conducted to identify which surfaces may be contaminated and the job categories that may contact these surfaces. Wipe samples were collected from potentially-contaminated surfaces and the hands of at-risk healthcare workers. Urine samples were collected from these same workers. Participants were asked to complete a questionnaire regarding their knowledge and usual protective habits regarding antineoplastic drugs and surveyed about contact with these agents on their work shift. Drug residual was measurable on surfaces located throughout the hospital medication system. Determinants associated with increased surface contamination were the drug preparation and drug administration stages of the medication system as well as having more job categories responsible for drug transport. Up to 11 job categories per facility may have an exposure risk and the maximum dermal contamination levels for every job category exceeded the limit of detection. Factors associated with increased dermal contamination were working in acute care hospitals, female personnel, working as a porter, nurse, transport, unit clerk or other roles in the drug administration unit and having a duty to handle antineoplastic drugs. Urinary drug contamination of participants was higher than in non-hospital controls confirming that exposure is occurring in the workplace. Being a pharmacy receiver, pharmacy technician, porter, nurse, or unit clerk and a facility having more job categories responsible for drug transport were associated with increased urinary contamination. This is believed to be the first study examining environmental contamination and occupational exposure to antineoplastic drugs across the entire hospital medication system.

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29

McPherson, John Peter. "DNA topoisomerase IIÃ, role in resistance to antineoplastic agents and induction of apoptosis." Thesis, National Library of Canada = Bibliothèque nationale du Canada, 1998. http://www.collectionscanada.ca/obj/s4/f2/dsk2/tape17/PQDD_0009/NQ35248.pdf.

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30

McCandless, Stewart Grant. "The synthesis of some novel 1,2,3-benzotriazine-platinum complexes with potential antineoplastic activity." Thesis, Heriot-Watt University, 1988. http://hdl.handle.net/10399/999.

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31

Baglioni, Michele <1977&gt. "Doxorubicina coniugata alla albumina umana lattosaminata: azione antineoplastica sui carcinomi epatocellulari indotti nel ratto dalla dietilnitrosammina." Doctoral thesis, Alma Mater Studiorum - Università di Bologna, 2009. http://amsdottorato.unibo.it/2147/.

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The experiments described in the thesis for my PhD were addressed to the study of the anticancer activity of a conjugate of doxorubicin (DOXO) with lactosaminated human albumin (L-HSA) on hepatocellular carcinomas (HCCs) induced in rats by diethylnitrosamine. L-HSA is a neoglycoprotein exposing galactosyl residues. The conjugate was prepared to improve the chemo therapeutic index of DOXO in the treatment of the well differentiated (WD) HCCs whose cells mantain the receptor for galactosyl terminating glycoproteins and consequently can actively internalize L-HSA. In my first experiments I found that L-HSA coupled DOXO produced concentrations of DOXO higher than those raised by an equal dose of free drug, not only in WD HCCs, but also in the poorly differentiated forms (PD) of these tumors which do no express the receptor for galactosyl terminating glycoproteins. Subsequently I provided evidence that penetration of L-HSA-DOXO in PD HCCs was due to a non-specific adsorption mediated by the DOXO residues of the conjugate which interact with the cell surface mainly because at physiological pH they are positively charged and bind to anionic phospholipids of the cell membrane. In subsequent experiments, by ultrasound technique, I studied the action of free and L-HSA coupled DOXO on the growth of rat HCCs. I found that L-HSA coupled DOXO hindered the development of new neoplastic nodules and inhibited the growth of the established tumors. In contrast, the free drug neither inhibited the development of HCCs nor prevented the growth of the established tumors. Moreover, the free drug produced a severe loss of weight of rats, a sign of severe toxicity, which was not caused by the conjugate. In conclusion assuming that the results obtained in rats can be applied to patients, the results of my thesis suggest that the conjugate by increasing the efficacy and tolerability of DOXO could improve the value of this drug in the treatment of human HCCs.

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32

Ganley, Brian Christopher. "Investigations into the chemical mechanisms of biological activity by heterocyclic di-N-oxides and 1,2 benzodithiolan-3-one 1-oxides /." free to MU campus, to others for purchase, 2000. http://wwwlib.umi.com/cr/mo/fullcit?p9999285.

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33

Hardy, Elizabeth Mary. "Pharmacokinetic and technical studies on novel administration routes for the antineoplastic antimetabolite 5-fluorouracil." Thesis, University of Exeter, 1995. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.296231.

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34

Claborn, Jordan, Moses Holleyman, and John B. Bossaer. "Consistency of Drug Information Resources in Identifying Drug-drug interactions with Oral Antineoplastic Agents." Digital Commons @ East Tennessee State University, 2017. https://dc.etsu.edu/etsu-works/2346.

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Targeted oral antineoplastic agents (OAs) have become a staple and rapidly growing field in the realm of cancer treatment. As with any chemotherapeutic/narrow spectrum agent, clinicians have to be aware of potential drug interactions that could interfere with therapy. Drug information databases are a common resource utilized to check for interactions between agents and patient's home medications. A major concern with OAs is that they are usually taken at home as well as picked up at a pharmacy by the patient themselves. With this kind of therapy adherence and patient side effect reporting becomes a concern. We wanted to determine the reliability of these databases for picking up potential interactions with patients on OAs. We accessed hospital records to find patients with various malignancies on OAs between the calendar year of 2013-2014, of which we found 876 that were screened for potential use of OAs. The goal was to find patients on OAs specifically and determine the number of drug interactions flagged by either drugs.com and/or Lexicomp®. In addition, the significance of the interaction as well as disagreements between databases were analyzed. A major interaction by Lexicomp® is defined as either a ‘D’ or an ‘X’ level interaction and on drugs.com is labeled ‘major.' Of the 876 screened we found 16 patients (one patient had tried 3 different agents, and another patient had tried two) on OAs. Lexicomp® flagged overall 42 interactions amongst all subjects, of which 17 were major interactions. Drugs.com flagged overall 44 interactions amongst all subjects, of which 11 were major interactions, being the more conservative of the two. Between the 2 databases there were 10 out of 18 major interactions that both were in agreement upon. These discrepancies are of concern in that clinicians hope that resources they utilize are incongruent with one another and allow them to practice in the safest manner in terms of avoided potential serious drug interactions whether it be harm to a patient or decreased effectiveness of the OA. Now that all patients have been screened, future research would be to determine the clinical significance of these interactions and whether or not they had an effect on patient outcomes.

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35

Clayborn, Jordan, Moses Holleyman, and John B. Bossaer. "Reliability of Drug Information Databases in Identifying Drug-drug Interactions with Oral Antineoplastic Agents." Digital Commons @ East Tennessee State University, 2016. https://dc.etsu.edu/etsu-works/2349.

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36

Doetsch, Natalie, Kimberly Harder-Ibarola, and Aliyah Sheth. "Exploration of Classic Confounders in Lymphoblastoid Cell Lines used to Study Select Antineoplastic Agents." The University of Arizona, 2010. http://hdl.handle.net/10150/623750.

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Class of 2012 Abstract
OBJECTIVES: Therapeutic response to chemotherapeutic agents in vitro can be studied using immortalized lymphoblastoid cell lines (LCLs). While LCLs provide a valuable model to study heritable factors and anticancer drug reponse in large populations, the results may be confounded by properties inherent to the model. This study is used to explore possible confounders in Choy et al.’s publicially available dataset (Accession#: GSE11582). METHODS: This study utilized Affymetrics U133A array gene expression and phenotypic data for 162 unrelated LCLs. SPSS was used for two-tailed bivariate Pearson correlation analysis comparing relative 6-mercaptopurine (6-MP), 5-fluorouracil (5-FU), and methotrexate sensitivities, growth rate and ATP levels. GeneSpring was used to compare the top and bottom quartiles of relative ATP levels using the unpaired T-test with a significance threshold of 0.001 and Benjamin-Hochberg FDR (n=82). RESULTS: It was found that relative sensitivities of 5-FU and 6-MP are significantly correlated (r2= 0.627, p<0.0001). Furthermore, it was determined that 5-FU sensitivity and growth rate and ATP levels are also correlated; however, no significant correlation was found between growth rate and ATP levles (r2=0.127, p=0.107). Relative ATP level was found to be a more significant determinant of 5-FU sensitivity than growth rate. GeneSpring analysis showed that 1500 genes are differentially regulated based on ATP levels. The gene ontology related to nucleic acid metabolism was overrepresented (p=1.425E-15). CONCLUSIONS: The results above suggest that growth rate and, to a greater extent, baseline ATP levels influence genetic expression of LCLs and may confound in vitro studies of antineoplastic agents.

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37

Sophie, Hamel. "Cardiovascular Effects and Pattern of Use of Antineoplastic Therapies in Female Breast Cancer Patients." Thesis, Université d'Ottawa / University of Ottawa, 2014. http://hdl.handle.net/10393/31523.

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Cancer survivors are at greater risk of cardiovascular diseases in comparison to the general population. Cardiovascular disorders are among the most prominent comorbidities in breast cancer patients. In order to gain a better understanding of the prescribing practices and cardiovascular risks associated with oncology drugs, this thesis encompasses a detailed review of the molecular and physiological mechanisms leading to drug‐induced cardiotoxicity and an evaluation of the cardiovascular risks associated with cancer drug therapies. Using a nested case‐control design, we evaluated whether these cancer drugs were associated with adverse cardiovascular outcomes under real‐world conditions of use. Although only few oncology drugs are indicated for breast cancer treatment, we were interested in prescribing practices and whether breast cancer treatments are restricted to labelled indications. The characterization of prescribing practices provides insights on the range of antineoplastic agents that should be considered in the evaluation of treatmentrelated adverse reactions such as cardiotoxicity. We found that selective estrogen receptor modulators demonstrated a better safety profile than aromatase inhibitors based on their mechanism of action on the cardiovascular system. These observations were corroborated by our findings from logistic regression analyses where aromatase inhibitors were associated with a higher risk of heart failure in a heterogeneous population of breast cancer patients. We reported that off‐label prescribing is common strategy in breast cancer treatment. While this practice tends to be associated with specific socio‐demographic and disease characteristics, the majority of off-label encounters are evidence‐based decisions. Because these off‐label treatments have their own inherent safety profiles, a comprehensive approach, covering all antineoplastic agents administered should be adopted in the evaluation of breast cancer treatment-induced cardiotoxicity. Careful monitoring of patients is crucial for the early detection of warning signs of cardiotoxicity to prevent long‐term deleterious effects. The information contained in this thesis provides useful considerations for the prospective surveillance of cancer drug‐induced cardiac events. These findings point to the need for a multi‐disciplinary approach to facilitate the rapid diagnosis and treatment of cardiac complications secondary to cancer therapy and to ensure that treatment decisions will maximize tumor response while minimizing adverse outcomes.

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38

Chenault, Darrell Vincent. "Total synthesis of 6-chlorodemethyllavendamycin esters and amides." Virtual Press, 1998. http://liblink.bsu.edu/uhtbin/catkey/1115748.

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The synthesis of several 6-Chlorodemethyllavendamycin analogs and their chemistry are described. In this investigation the following compounds were prepared:6-Chlorodemethyllavendamycin methyl ester, 6-Chlorodemethyllavendamycin ethylester, 6-Chlorodemethyllavendamycin butyl ester, 6-Chlorodemethyllavendamycin isoamyl ester, 6-Chlorodemethyllavendamycin octyl ester, and 6-Chlorodemethyllavendamycin amide. Pictet Spengler condensation of 7-amino-6-chloro-2-formylquinoline-5,8-dione with tryptophan methyl ester, tryptophan ethyl ester, tryptophan butyl ester, tryptophan isoamyl ester, tryptophan octyl ester, and tryptophan amide in anisole afforded the compounds. 7-amino-6-chloro-2-formylquinoline-5,8-dione was prepared according to the following general procedures.The first step is the nitration of 8-Hydroxy-2-methylquinoline. 8-Hydroxy-2methylquinoline is reacted with 70% mixture of HNO3/H2SO4 to produce 5,7-dinitro-8hydroxy-2-methylquinoline. The next step requires hydrogenation and acylation. 5,7Dinitro-8-hydroxy-2-methylquinoline was reduced by H2/Pd-C in the presence of HCl and H20 filtered and then treated with sodium sulfite, sodium acetate and acetic anhydride to yield 5,7-diacetamido-8-acetoxy-2-methylquinoline. 5,7-Diacetamido-8-acetoxy-2methylquinoline was oxidized by potassium dichromate to produce 7-acetamido-2methylquinoline-5,8-dione. 7-Acetamido-2-methylquinoline-5,8-dione was chlorinated using hydrogen chloride gas in dry methanol producing 7-amino-6-chloro-2methylquinoline-5,8-dione. Treatment of 7-amino-6-chloro-2-methylquinoline-5,8-dione with selenium dioxide, under reflux in 1,4-dioxane produced 7-amino-6-chloro-2formylquinoline-5, 8-dione.All structures were confirmed by 'H NMR, IR, EIMS, and HRMS.
Department of Chemistry

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39

Reese, Michael. "Drug design (STAT5 modulators), development (Glyceollin I) and improvement (Esmolol Plus) /." Connect to full text in OhioLINK ETD Center, 2009. http://rave.ohiolink.edu/etdc/view?acc%5Fnum=toledo1265033116.

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Thesis (M.S.)--University of Toledo, 2009.
Typescript. "Submitted as partial fulfillment of the requirements for the Master of Science Degree in Medicinal Chemistry." "A thesis entitled"--at head of title. Bibliography: leaves 45-48.

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40

Masquelier, Michèle. "Leukemia chemotherapy : experimental studies on pharmacological optimisation /." Stockholm, 2004. http://diss.kib.ki.se/2004/91-7140-046-X/.

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41

Eskens, D., and A. Gardner. "Specificity and Sensitivity of Drug Interaction Databases to Detect Meaningful QTc Interactions with Oral Antineoplastics." Digital Commons @ East Tennessee State University, 2019. https://dc.etsu.edu/etsu-works/7800.

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42

Chen, Chang-Shi. "Beyond induction of histone acetylation the multi-facets of the antineoplastic effect of HDAC inhibitors /." Columbus, Ohio : Ohio State University, 2006. http://rave.ohiolink.edu/etdc/view?acc%5Fnum=osu1164649581.

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43

Permana, Paskasari A. "SV40 minichromosome: A mammalian replicon model for investigations of antineoplastic drugs and DNA damaging agents /." The Ohio State University, 1993. http://rave.ohiolink.edu/etdc/view?acc_num=osu1487846885776862.

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44

Hendrix, Martin. "Synthetic approaches toward pancratistatin." Thesis, Georgia Institute of Technology, 1993. http://hdl.handle.net/1853/27300.

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45

Lin, Tung Yin. "Synthetic studies towards the stellettins /." View online, 2008. http://repository.eiu.edu/theses/docs/32211131443971.pdf.

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46

David, Wendi Marjene. "Studies of a new class of aza-enediynes : aza-Bergman cyclization and the potential use of aza-enediynes as antitumor agents /." Full text (PDF) from UMI/Dissertation Abstracts International, 2000. http://wwwlib.umi.com/cr/utexas/fullcit?p3004248.

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47

Fellows, Ingrid Maria. "A formal synthesis of FR-900482 and studies toward the total synthesis of FR-900482 /." Digital version accessible at:, 1999. http://wwwlib.umi.com/cr/utexas/main.

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48

Ekborn, Andreas. "Cisplatin induced ototoxicity : pharmacokinetics, prediction and prevention /." Stockholm, 2003. http://diss.kib.ki.se/2003/91-7349-721-5.

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49

Erdal, Hamdiye. "Characterization of the mechanisms of action of anticancer agents in vitro and monitoring their effects in vivo /." Stockholm, 2005. http://diss.kib.ki.se/2005/91-7140-202-0/.

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50

Lineswala, Jayana P. "Total synthesis of lavendamycin amides." Virtual Press, 1996. http://liblink.bsu.edu/uhtbin/catkey/1036197.

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The synthesis of 7-N-acetyldemethyllavendamycin butyl amide (47), 7-Nacetyldemethyllavendamycin isopropyl amide (48), 7-N-acetyldemethyllavendamycin amide of piperidine (49), 7-N-acetyldemethyllavendamycin amide of pyrrolidine (50), 7N-acetyldemethyllavendamycin amide of morpholine (51), demethyllavendamycin butyl amide (52), demethyllavendamycin amide of pyrrolidine (53), and demethyllavendamycin amide of morpholine (54) are described. Pictet Spengler condesation of 7-acetamido-2formylquinoline-5,8-dione (28) with tryptophan butyl amide (66), tryptophan isopropyl amide (67), tryptophan amide of piperidine (68), tryptophan amide of pyrrolidine (69), and tryptophan amide of morpholine (70) in an anisole - pyridine solution directly afforded the five lavendamycin amides 47-51. Compounds 52, 53, and 54 were obtained by hydrolysis of 47, 50, and 51 with 70% H2SO4-H20 solution.Aldehyde 28 was prepared according to the following general procedure.Nitration of 8-hydroxy-2-methylquinoline (30) yielded 8-hydroxy-2-methyl-5,7 dinitroquinoline (31). Compound 31 was then hydrogenated and acylated with acetic anhydride to yield 5,7-diacetamido-2-methyl-8-acetoxyquinoline (33). Compound 33 was oxidized by potassium dichromate to give 7-acetamido-2-methylquinoline-5,8-dione (27). Treatment of 27 with selenium dioxide in refluxing 1,4-dioxane afforded compound 28.Compounds 66, 67, 68, 69, and 70 were synthesized from compounds 61,62, 63, 64, and 65. These compounds were deprotected with ammonium formate in the presence of 10% Palladium on charcoal in methanol under an argon balloon at atmospheric pressure.Compounds 61, 62, 63, 64, and 65 were obtained from 58 with butylamine, isopropylamine, piperidine, pyrrolidine, and morpholine respectively in the presence of triethylamine under an argon balloon at atmospheric pressure.Compound 58 was synthesized by the reaction of N-carbobenzyloxytryptophan, with N-hydroxy succinimide, in the presence of N-dicyclohexylcarbodimide in dried and distilled dioxane under an argon balloon at atmospheric pressure.The structures of the novel compounds 58, 47, 48, 49, 50, 51, 52, 53, and 54 were confirmed by 1H NMR, IR, EIMS, and HRMS.The structures of protected and deprotected amides 61, 62, 63, 64, 65, 66, 67, 68, 69, and 70 were also confirmed by 1 H NMR and IR spectroscopy.
Department of Chemistry

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Dissertations / Theses on the topic 'Antineoplastika'

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