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Articles de revues sur le sujet "Potent anti-cancer agent"

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Bhat, Smitha S., Shashanka K. Prasad, Chandan Shivamallu, Kollur Shiva Prasad, Asad Syed, Pruthvish Reddy, Charley A. Cull et Raghavendra G. Amachawadi. « Genistein : A Potent Anti-Breast Cancer Agent ». Current Issues in Molecular Biology 43, no 3 (10 octobre 2021) : 1502–17. http://dx.doi.org/10.3390/cimb43030106.

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Genistein is an isoflavonoid present in high quantities in soybeans. Possessing a wide range of bioactives, it is being studied extensively for its tumoricidal effects. Investigations into mechanisms of the anti-cancer activity have revealed many pathways including induction of cell proliferation, suppression of tyrosine kinases, regulation of Hedgehog-Gli1 signaling, modulation of epigenetic activities, seizing of cell cycle and Akt and MEK signaling pathways, among others via which the cancer cell proliferation can be controlled. Notwithstanding, the observed activities have been time- and dose-dependent. In addition, genistein has also shown varying results in women depending on the physiological parameters, such as the early or post-menopausal states.
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Ibrahim, Mona, Donia Wafaa et Ghada El Nady. « Ginger Extract as Potent Anti-Cancer Agent against Breast Cancer ». Journal of Agricultural Chemistry and Biotechnology 13, no 12 (1 décembre 2022) : 139–43. http://dx.doi.org/10.21608/jacb.2023.183821.1042.

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SAXENA, B., L. ZHU, M. HAO, E. KISILIS, M. KATDARE, O. OKTEM, A. BOMSHTEYN et P. RATHNAM. « Boc-lysinated-betulonic acid : A potent, anti-prostate cancer agent ». Bioorganic & ; Medicinal Chemistry 14, no 18 (15 septembre 2006) : 6349–58. http://dx.doi.org/10.1016/j.bmc.2006.05.048.

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Samuel, Samson, Elizabeth Varghese, Peter Kubatka, Chris Triggle et Dietrich Büsselberg. « Metformin : The Answer to Cancer in a Flower ? Current Knowledge and Future Prospects of Metformin as an Anti-Cancer Agent in Breast Cancer ». Biomolecules 9, no 12 (9 décembre 2019) : 846. http://dx.doi.org/10.3390/biom9120846.

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Interest has grown in studying the possible use of well-known anti-diabetic drugs as anti-cancer agents individually or in combination with, frequently used, chemotherapeutic agents and/or radiation, owing to the fact that diabetes heightens the risk, incidence, and rapid progression of cancers, including breast cancer, in an individual. In this regard, metformin (1, 1-dimethylbiguanide), well known as ‘Glucophage’ among diabetics, was reported to be cancer preventive while also being a potent anti-proliferative and anti-cancer agent. While meta-analysis studies reported a lower risk and incidence of breast cancer among diabetic individuals on a metformin treatment regimen, several in vitro, pre-clinical, and clinical studies reported the efficacy of using metformin individually as an anti-cancer/anti-tumor agent or in combination with chemotherapeutic drugs or radiation in the treatment of different forms of breast cancer. However, unanswered questions remain with regards to areas such as cancer treatment specific therapeutic dosing of metformin, specificity to cancer cells at high concentrations, resistance to metformin therapy, efficacy of combinatory therapeutic approaches, post-therapeutic relapse of the disease, and efficacy in cancer prevention in non-diabetic individuals. In the current article, we discuss the biology of metformin and its molecular mechanism of action, the existing cellular, pre-clinical, and clinical studies that have tested the anti-tumor potential of metformin as a potential anti-cancer/anti-tumor agent in breast cancer therapy, and outline the future prospects and directions for a better understanding and re-purposing of metformin as an anti-cancer drug in the treatment of breast cancer.
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Purushottamachar, Puranik, Aakanksha Khandelwal, Tadas S. Vasaitis, Robert D. Bruno, Lalji K. Gediya et Vincent C. O. Njar. « Potent anti-prostate cancer agents derived from a novel androgen receptor down-regulating agent ». Bioorganic & ; Medicinal Chemistry 16, no 7 (1 avril 2008) : 3519–29. http://dx.doi.org/10.1016/j.bmc.2008.02.031.

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Sameem, Bilqees, Ebrahim Saeedian Moghadam, Majid Darabi, Zahra Shahsavari et Mohsen Amini. « Triarylpyrazole Derivatives as Potent Cytotoxic Agents ; Synthesis and Bioactivity Evaluation “Pyrazole Derivatives as Anticancer Agent” ». Drug Research 71, no 07 (19 mai 2021) : 388–94. http://dx.doi.org/10.1055/a-1498-1714.

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Abstract Background During the last recent years, several anti-cancer agents were introduced for the treatment of diverse kinds of cancer. Despite their potential in the treatment of cancer, drug resistance and adverse toxicity such as peripheral neuropathy are some of the negative criteria of anti-cancer agents and for this reason, the design and synthesis of new anti-cancer agents are important. Objective Design, synthesis, and anticancer activity evaluation of some pyrazole derivatives. Methods A series of Target compounds were prepared using multistep synthesis. Their cytotoxic activity against three different human cancer cell lines namely human colon carcinoma cells (HT-29), epithelial carcinoma cells (U-87MG), pancreatic cancerous cells (Panc-1) as well as AGO1522 normal cell line using in vitro 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay was investigated. Results 1,3-Diaryl-5-(3,4,5-trimethoxyphenyl)-4,5-dihydro-1H-pyrazole and 1,3-Diaryl-5-(3,4,5-trimethoxyphenyl)- 1H-pyrazole were synthesized in good yields and their structure and purity were confirmed using 1H-NMR, 13C-NMR, and elemental analysis. Generally, the synthesized scaffolds exhibited good cytotoxicity against cancerous cell lines in comparison to the reference standard, paclitaxel. Compounds 3a and 3c, in Annexin V/ PI staining assay, exerted remarkable activity in apoptosis induction in HT-29 cell lines. Both of them also led to cell cycle arrest in the sub-G1 phase which is inconsistent with the results of apoptosis assay. Conclusion Concerning obtained results, it is interesting to synthesis more pyrazole derivatives as anticancer agents.
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Watanabe, Coran M. H., Lubica Supekova et Peter G. Schultz. « Transcriptional Effects of the Potent Enediyne Anti-Cancer Agent Calicheamicin γ1I ». Chemistry & ; Biology 9, no 2 (février 2002) : 245–51. http://dx.doi.org/10.1016/s1074-5521(02)00103-5.

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Tundis, Rosa, Jayanta Kumar Patra, Marco Bonesi, Subrata Das, Rajat Nath, Anupam Das Talukdar, Gitishree Das et Monica Rosa Loizzo. « Anti-Cancer Agent : The Labdane Diterpenoid-Andrographolide ». Plants 12, no 10 (12 mai 2023) : 1969. http://dx.doi.org/10.3390/plants12101969.

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In spite of the progress in treatment strategies, cancer remains a major cause of death worldwide. Therefore, the main challenge should be the early diagnosis of cancer and the design of an optimal therapeutic strategy to increase the patient’s life expectancy as well as the continuation of the search for increasingly active and selective molecules for the treatment of different forms of cancer. In the recent decades, research in the field of natural compounds has increasingly shifted towards advanced and molecular level understandings, thus leading to the development of potent anti-cancer agents. Among them is the diterpene lactone andrographolide, isolated from Andrographis paniculata (Burm.f.) Wall. ex Nees that showed shows a plethora of biological activities, including not only anti-cancer activity, but also anti-inflammatory, anti-viral, anti-bacterial, neuroprotective, hepatoprotective, hypoglycemic, and immunomodulatory properties. Andrographolide has been shown to act as an anti-tumor drug by affecting specific molecular targets that play a part in the development and progression of several cancer types including breast, lung, colon, renal, and cervical cancer, as well as leukemia and hepatocarcinoma. This review comprehensively and systematically summarized the current research on the potential anti-cancer properties of andrographolide highlighting its mechanisms of action, pharmacokinetics, and potential side effects and discussing the future perspectives, challenges, and limitations of use.
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Liu, Weiya, Eugene K. Lee, Karim Pirani, Brian S. J. Blagg et Jeffrey M. Holzbeierlein. « A new HSP90 inhibitor as therapeutic agent for bladder cancer. » Journal of Clinical Oncology 35, no 6_suppl (20 février 2017) : 416. http://dx.doi.org/10.1200/jco.2017.35.6_suppl.416.

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416 Background: Hsp90 represents one of the most promising biological targets for the treatment of cancer, including bladder cancer. A number of Hsp90 inhibitors that target the N-terminal ATP-binding pocket have demonstrated potent antiproliferative effects. However, a major drawback is that they induce a prosurvival heat shock response (HSR). We demonstrate the effects of a novel Hsp90 beta selective inhibitor on bladder cancer cells, which shows potent antiproliferative effects without inducing HSR. Methods: Cell Titer-Glo luminescent anti-proliferative assay was used to determine the IC50 numbers in UC3 cells. Trypan Blue Cytotoxicity assay was performed for 24h treatment with increasing concentrations of the inhibitor. Effects of the cmpound on Hsp90’s client protein degradation were investigated by Western Blot. Results: This new compound exhibits potent anti-proliferative in bladder cancer cells. IC50 number is determined as 0.30 µM for UC3 cancer cells. The toxicity assay was also performed over UC3 cells at 24h.1uM KU new compound has the similar effects on UC3 cells as 10 uM 17AAG: inhibit the cancer cells growth to half, but maintain over 60% viability of the cells. The western blot were also performed over UC3 cells, and some new target proteins such as FGFR3 and PKM2 were investigated. The data showed that, this new compound would not induce the heat shock response like 17AAG (Hsp27), and did cause some Hsp90β related protein degradation (CXCR4). FGFR3, PKM2, Her2, Hsf-1and B-raf all show degradation to different extent. Conclusions: A novel Hsp90 inhibitor, exhibits potent anti-proliferative and cytotoxic activity along with client protein degradation, without induction of HSR in bladder cancer cell lines. The reduction of Hsp90 beta related client protein caused by this compound suggests the potential to develop isoform specific inhibitors of Hsp90 for better antitumor therapies.
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Rosenthal, Gerald A. « l-Canaline : A potent antimetabolite and anti-cancer agent from leguminous plants ». Life Sciences 60, no 19 (avril 1997) : 1635–41. http://dx.doi.org/10.1016/s0024-3205(96)00595-4.

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Thèses sur le sujet "Potent anti-cancer agent"

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Afolabi, Fatai. « Synthesis of novel fluorescence cationic gold(I) complexes as potent anti-cancer agent ». Thesis, University of Sussex, 2018. http://sro.sussex.ac.uk/id/eprint/80482/.

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Madadi, Nikhil Reddy. « Synthesis and Biological Evaluation of Novel Resveratrol and Combretastatin A4 Derivatives as Potent Anti-Cancer Agents ». UKnowledge, 2014. http://uknowledge.uky.edu/pharmacy_etds/42.

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Resveratrol has been reported as a potential anticancer agent but cannot be used as an antitumor drug due to its chemical and metabolic instability. We have designed and synthesized 184 novel compounds related to resveratrol in an attempt to produce more potent and drug-like molecules. We have identified a tetrazole analog of resveratrol, ST-145(a) as a lead anticancer agent from the resveratrol analog series of compounds with a GI50 value of less than 10nM against almost all the human cancer cell lines in the National Cancer Institute’s screening panel. In a separate study, we tested the hypothesis that the limited bioavailability of resveratrol, can be improved by synthesizing analogs which would be glucuronidated at a lower rate than resveratrol itself. We demonstrated that ST-05 and ST-12(a) exhibit lower glucuronidation profiles when compared to resveratrol and that these synthesized stilbenoids likely represent useful scaffolds for the design of efficacious resveratrol analogs. We have also initiated a new discovery program to identify selective CB1 and CB2 receptor ligands from a library of novel stilbene scaffolds structurally related to the resveratrol molecule. From the screened resveratrol analogs, two compounds were identified as selective CB2 and CB1 ligands. Compound ST-179 had 47-fold selectivity for CB2 (Ki = 284 nM) compared to CB1, while compound ST-160 was 2-fold selective for CB1 (Ki = 400 nM) compared to the CB2 receptor. These structural analogs have the potential for development as novel cannabinoid therapeutics for treatment of obesity and/or drug dependency. Combretastatin A4 (CA-4) is one of the most potent antiangiogenic and antimitotic agents of natural origin. However, CA-4 suffers from chemical instability due to cis-trans isomerism in solution. To circumvent this problem, we have developed a facile procedure for the synthesis of novel 4,5-diaryl-2H-1,2,3-triazoles as CA-4 analogs to constrain the molecule to its cis-configuration. Twenty three triazoles were prepared as CA-4 analogs and submitted for anticancer screening. Among these CA-4 analogs, ST-467 and ST-145(b) can be considered as lead anticancer agents from this series, and further investigation against various cancer cell types in vivo with this class of compound may provide novel therapeutic avenues for treatment.
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Chapitres de livres sur le sujet "Potent anti-cancer agent"

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De Pauw, Ines, Carolien Boeckx et An Wouters. « Mechanisms of Cetuximab Resistance and How to Overcome It ». Dans Critical Issues in Head and Neck Oncology, 21–51. Cham : Springer International Publishing, 2021. http://dx.doi.org/10.1007/978-3-030-63234-2_3.

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AbstractDeregulated or increased signalling of the epidermal growth factor receptor (EGFR) plays an integral role in the development of various cancer types, including head and neck squamous cell carcinoma (HNSCC), making it a compelling drug target. However, after initially promising results of EGFR-targeted therapies, such as the monoclonal antibody cetuximab, it became clear that both intrinsic and acquired therapeutic resistance are major roadblocks in the field of personalised cancer treatments.In order to unravel and overcome resistance to cetuximab, at least two strategies can be adopted.Firstly, therapeutic resistance to anti-EGFR therapy may arise from mechanisms that can compensate for reduced EGFR signalling and/or mechanisms that can modulate EGFR-dependent signalling. In this chapter, we discuss which mechanisms of cetuximab resistance are already known and which ones deserve further investigation. This enhanced knowledge will guide us to rationally design and test novel combination therapies that overcome resistance to EGFR-targeting agents in cancer treatment.Secondly, an urgent need remains to develop novel targeted treatments for single-agent or combined therapy use. In this view, due to the particular mode of activation of the EGFR receptor, involving ligand-induced homo- and heterodimerization of the four HER receptors, an increased inhibition scope of HER receptors most likely results in a more potent blockade of the HER network, preventing premature emergence of resistance and leading to a more pronounced therapeutic benefit. We discuss two multitargeted compounds, being MEHD7945A (duligotuzumab) and afatinib, in this chapter.Despite the huge efforts to unravel the molecular landscape of HNSCC, the main clinically validated target remains EGFR. However, immune checkpoints, like programmed cell death protein 1 (PD-1), are gaining clinical approvals as well. We underscore the importance of adopting rational drug combinations to enhance the therapeutic effect of the EGFR-inhibitor cetuximab and highlight the ongoing search for predictive biomarkers, with the ultimate goal of delivering individualized cancer therapy to HNSCC patients.
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Friedman, Paula N., Dana F. Chace, Susan L. Gawlak et Clay B. Siegall. « The Single-Chain Immunotoxins BR96 sFv-PE40 and BR96 sFv-PE38 : Potent Anti-Tumor Agents for the Treatment of Human Cancer ». Dans Growth Factors, Peptides and Receptors, 409–14. Boston, MA : Springer US, 1993. http://dx.doi.org/10.1007/978-1-4615-2846-3_39.

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Cheng, Yu-Chen, Yu-Chiang Hung et Wen-Long Hu. « Polyphenols of Salvia miltiorrhiza in Aging-Associated Cardiovascular Diseases and Cancer ». Dans Phenolic Compounds [Working Title]. IntechOpen, 2021. http://dx.doi.org/10.5772/intechopen.98632.

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With the increasing lifespan of human, cardiovascular diseases (CVDs) and cancer are the main diseases leading to the death in the world. Aging is related to a progressive decline in cardiovascular function and structure. While human body suffer from oxidative stress, reactive oxygen species (ROS) are generated as metabolic by-products, which lead to inactivate proteins, damage nucleic acids, and alter the fatty acids of lipids. The accumulation of this oxidative damage contributes to the development of heart disease, diabetes, chronic inflammatory diseases, and cancer. Polyphenols have been widely studied as an anti-oxidant agent in the world. Danshen, the dried root or rhizome of Salvia miltiorrhiza Bunge. is a common Traditional Chinese medicine used in cardiovascular disease and cancer. The main polyphenols in Danshen are phenolic acids (including Salvianolic acids A and B, rosmarinic acid, and their derivatives) and flavonoids. Salvianolic acids have potent anti-oxidative capabilities due to their polyphenolic structure and exhibit cardiovascular protection through mechanisms of ROS scavengers, reduction of leukocyte-endothelial adherence, inhibition of inflammation and indirect regulation of immune function. Salvianolic acids A and B have been reported to owe anti-cancer, anti-inflammatory activities not only through inducing apoptosis, halting cell cycle and adjourning metastasis by targeting multiple deregulated signaling networks of cancer but also sensitizing cancer cells to chemotherapeutic agents.
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« Tripentones : A Promising Series of Potent Anti-Cancer Agents ». Dans Advances in Anticancer Agents in Medicinal Chemistry, sous la direction de Christophe Rochais, Sylvain Rault et Patrick Dallemagne, 313–43. BENTHAM SCIENCE PUBLISHERS, 2013. http://dx.doi.org/10.2174/9781608054961113020009.

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Sadik, Saabira Banu Sahubar, Prathibha Sivaprakasam, Nishanthi Ramasami et Ashok Kumar Pandurangan. « The Molecular Mechanisms Involved in Suppressing Triple Negative Breast Cancer Using Natural Agents ». Dans Handbook of Research on Natural Products and Their Bioactive Compounds as Cancer Therapeutics, 45–71. IGI Global, 2022. http://dx.doi.org/10.4018/978-1-7998-9258-8.ch003.

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Breast cancer is an aggressive and primary cause of death among women globally. Triple negative breast cancer (TNBC) is one of the sub types of breast cancer. TNBC lacks the expression of progesterone receptor (PR), estrogen receptor (ER), and human epidermal factor 2 (HER2), which leads to poor diagnosis resulting in lack of targeted therapies. On the other hand, natural products are also cost efficient, non-toxic, and abundantly available in nature. Natural products have also been reported to exert various pharmacological activities including cardioprotective, anti-diabetic, antimicrobial, anti-inflammatory, etc. In this chapter, summarization of 12 well known natural products such as chebulinic acid, maslinic acid, apigenin, piperlongumine, Liquiritigenin, berberine, icariin, bufalin, which are targeted against TNBC through regulation of different pathways, and their mechanism are briefly explained. These natural products are already used to treat various diseases at the preclinical level and also have shown to have effective anti-tumor effect and can act as potent anti-TNBC agents.
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Dwarka, Depika, Himansu Baijnath et John Jason Mellem. « Bioactive Compounds as Therapeutic Intervention in Cancer Therapy ». Dans Therapeutic Use of Plant Secondary Metabolites, 84–110. BENTHAM SCIENCE PUBLISHERS, 2022. http://dx.doi.org/10.2174/9789815050622122010007.

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Neither transmittable nor communicable, painstakingly the second most fataldisease worldwide, cancer has gained the interest of scientists who are attempting withtenacity to decrypt its unknown facets, discover new diagnosis techniques, as well as tocreate improved and more efficient treatment methods. A major impediment toeffective cancer therapy is the inability to destroy the complete malignant tumourgrowth and evolution of tumour resistance. Chemotherapeutic drugs are known fortheir cell death mode of action, thereby incapacitating non-cancerous cells in theprocess. A successful anti-cancer drug should kill or debilitate cancer cells withoutcausing unnecessary damage to normal cells. Administration of natural bioactivecompounds exemplifies an alternative technique as they are associated with lowertoxicities. These bioactive molecules are effective and demonstrate great specificity asthey possibly operate as potent anti-oxidants and apoptosis inducers. Moderatingapoptosis might be helpful in managing, treating, or deterring cancer. Significantly,bioactive compounds are providing such templates. Plants have a long history in cancertreatment. More than 3000 species have been known for their anti-cancer potential.Over 60% of currently used anti-cancer agents are derived in one way or another fromhigher plants. This chapter describes the roles and advancements of the use of bioactivecompounds in the treatment of cancer.
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Chauhdary, Zunera, Muhammad Ajmal Shah, Malik Hassan Mehmood, Uzma Saleem, Azhar Rasul, Ghulam Mujtaba Shah, Ajmal Khan, Ahmed Al-Harrasi, Shabnoor Iqbal et Shabana Bibi. « Saponins in the Treatment of Gastrointestinal Tract Cancer ». Dans Phytonutrients in the Treatment of Gastrointestinal Cancer, 159–81. BENTHAM SCIENCE PUBLISHERS, 2023. http://dx.doi.org/10.2174/9789815049633123010010.

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The natural glycosides with triterpenoid or spirostaneaglycones are the saponins, which are associated with a wide range of therapeutic activities, inclusive of gastrointestinal anticancer activities. To promote research and development of novel cytotoxic agents against GIT cancer, this chapter focused on the anticancer potentia l of the naturally occurring triterpenoid and steroidal saponins. The in vitro assays and in vivo studies authenticated the anticancer potential of these compounds through anti-angiogenic, anti-proliferative, anti-metastatic and anti-multidrug resistance activities. The protein targets and signaling cascades behind the anticancer effect of these compounds in GIT cancer are also discussed in this chapter.
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Sarkar, Arnab, Tanmoy Banerjee, Avik Maji, Abhik Paul et Tanmoy Guria. « Mikania Species : Revealing Phytochemicals from the Pandora’s Box ». Dans New Avenues in Drug Discovery and Bioactive Natural Products, 149–67. BENTHAM SCIENCE PUBLISHERS, 2023. http://dx.doi.org/10.2174/9789815136326123020009.

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Natural medicines and traditional remedies are pretty valuable. Ayurveda, Traditional Chinese medicine, and Unani have all been practised in various parts of the world and have grown into well-organized medical systems. Secondary metabolites such as alkaloids, flavonoids, and tannins have already established their anti-microbial, anti-diabetic, and anti-cancer attributes. Mikania is one such plant genus used in folk medicine, which belongs to the Asteraceae family and is native to Central and South America. Still, it is extensively dispersed in Southeast Asia and Pacific Islands. Phytometabolites, viz., mikanolides and achalensolide, have emerged as potent antineoplastic agents. Sesquiterpene lactones such as deoxymikanolide and mikanolide possess anti-microbial activities. Apart from sesquiterpenes, several phenolic compounds comprising (+)-isolariciresinol and protocatechuic aldehyde were found in the aerial parts of Mikania micrantha. Antifungal activity of essential oil containing β.caryophyllene, δ-cadinene, and α-cubebene was characterized by GC/MS and isolated from Mikania scandens. Various steroids and diterpenoids obtained from Mikania cordata exhibited potent analgesic activity. This plant also contains germacrene D, β.pinene, and α-thujene, characterized by GC/MS. Many phenylpropanoids, sesquiterpenes, and diterpenes obtained from Mikania laevigata were characterized using NMR and mass spectrometry. Lupeol, lupeol acetate, and kaurene diterpenes were derived from Mikania glomerata and validated using RP-HPLC methods.
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Bachar, Sitesh C., A. K. M. Shafiul Kadir, S. M. Riajul Wahab et Abdullah Al Hasan. « Heterocyclic Anti-cancer Compounds Derived from Natural Sources with their Mechanism of Action ». Dans Key Heterocyclic Cores for Smart Anticancer Drug–Design Part I, 1–56. BENTHAM SCIENCE PUBLISHERS, 2022. http://dx.doi.org/10.2174/9789815040074122010004.

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The variety of natural compounds is indispensable due to their mechanism of action. For many years, natural compounds have been used to develop new classes of chemotherapeutic agents. Chemotherapeutic agents derived and synthesised from natural sources could be the best possible alternatives to minimise the harmful after effects of conventionally used agents against cancer, especially oral and maxillofacial carcinoma and tumors. The proposed chapter concentrates on recent research on various classes of natural scaffolds and their analogues that possess potent antitumor activity. Moreover, we would like to provide an analysis of preclinical and/or clinically investigated natural compounds. These compounds and their synthetic heterocyclic analogues were found to be obtained through bioactivity and mechanism of action directed isolation and characterization, conjoined with modification using rational drug design-based approaches and analogue synthesis. Structure-activity relationships, structural change, and molecular mechanisms of action will all be examined.
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Haider, Kashif, et Mohammad Shahar Yar. « Advances of Benzimidazole Derivatives as Anticancer Agents : Bench to Bedside ». Dans Benzimidazole [Working Title]. IntechOpen, 2022. http://dx.doi.org/10.5772/intechopen.101702.

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Benzimidazole is one of the privileged nitrogen-containing scaffolds known for its versatile diversified role in insecticides, pesticides, dyes, pigments and pharmaceuticals. Due to its electron-rich environment, structural features and binding potency of various therapeutic targets, benzimidazole derivatives exhibit a broad spectrum of biological activity that majorly includes antimicrobial, antifungal, analgesics, anti-diabetic and anticancer agents. Several benzimidazole scaffolds bearing drugs are clinically approved; they are used for various indications. For example, Bilastine, Lerisetron, Maribavir and Nocodazole are the most widely used benzimidazole-based marketed drugs available as an antihistamine, antiviral and antimitotic agent, respectively. Another example is the recently approved anticancer drug Binimetinib and Selumetinib, which are indicated for BRAF mutated melanoma and plexiform neurofibromas. Not only this, many benzimidazole-based anticancer drugs are in late phases of clinical development. Due to the vast therapeutic potential of benzimidazole scaffold in cancer research, medicinal chemists have gained a lot of attraction to explore it more and develop novel, highly effective and target-specific benzimidazole-based potential anticancer drugs.
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Actes de conférences sur le sujet "Potent anti-cancer agent"

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Vakkalanka, Swaroop, Kanthikiran Varanasi, Sridhar Veeraraghavan, Meyyappan Muthuppalaniappan, Gayatriswaroop Merikapudi, Sumalatha Kuppireddi et Srikant Viswanadha. « Abstract 2599 : RP3035, a potent cytostatic anti-cancer agent, reduces NCI-H460 tumor growth in mice via inhibition of Orai1 ». Dans Proceedings : AACR 102nd Annual Meeting 2011‐‐ Apr 2‐6, 2011 ; Orlando, FL. American Association for Cancer Research, 2011. http://dx.doi.org/10.1158/1538-7445.am2011-2599.

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Guo, Peng, Jiang Yang, Marsha Moses et Debra Auguste. « Abstract 4410 : An ICAM-1-targeted, Lcn2 siRNA-encapsulating liposome as a potent anti-angiogenic agent for triple-negative breast cancer ». Dans Proceedings : AACR 106th Annual Meeting 2015 ; April 18-22, 2015 ; Philadelphia, PA. American Association for Cancer Research, 2015. http://dx.doi.org/10.1158/1538-7445.am2015-4410.

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Tanaka, Nozomu, Yukari Yamada, Akio Fujioka, Keisuke Yamamura, Satoko Ito, Kenichi Matsuo et Teruhiro Utsugi. « Abstract B86 : Potent antitumor effect of TAS-102, a novel oral anti-neoplastic nucleoside agent, on both cetuximab-sensitiveKRASwild-type and cetuximab-resistantKRASmutated colorectal cancer cells via trifluorothymidine incorporation into DNA. » Dans Abstracts : AACR-NCI-EORTC International Conference : Molecular Targets and Cancer Therapeutics--Oct 19-23, 2013 ; Boston, MA. American Association for Cancer Research, 2013. http://dx.doi.org/10.1158/1535-7163.targ-13-b86.

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Pollard, John R. « Abstract IA11 : Discovery and characterization of potent and selective inhibitors of ATR kinase as anti-cancer agents ». Dans Abstracts : AACR Precision Medicine Series : Targeting the Vulnerabilities of Cancer ; May 16-19, 2016 ; Miami, FL. American Association for Cancer Research, 2017. http://dx.doi.org/10.1158/1557-3265.pmccavuln16-ia11.

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Wang, Shunyou, Lucy Lan, Mathew Janes, Katti Jessen, Linda Kessler, Jeff Kucharski, Xin Xin Guo et al. « Abstract 3753 : Potent anti-tumor activity of mTOR kinase inhibitor in combination with anti-angiogenic agents in preclinical models of renal cell cancer ». Dans Proceedings : AACR 103rd Annual Meeting 2012‐‐ Mar 31‐Apr 4, 2012 ; Chicago, IL. American Association for Cancer Research, 2012. http://dx.doi.org/10.1158/1538-7445.am2012-3753.

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Irie, Hiroki, Kei Oguchi, Kimihiro Ito, Yayoi Fujioka, Yuichi Kawai, Tadashi Shimamura, Hikari Araki et al. « Abstract B179 : TAS0728, a HER2-selective covalent inhibitor, demonstrates potent antitumor effect as a single agent and in combination with anti-HER2 antibodies in HER2-overexpressed tumor models ». Dans Abstracts : AACR-NCI-EORTC International Conference : Molecular Targets and Cancer Therapeutics ; October 26-30, 2017 ; Philadelphia, PA. American Association for Cancer Research, 2018. http://dx.doi.org/10.1158/1535-7163.targ-17-b179.

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Parab, Mala, Pramodkumar Gupta, Shruti Chandrashekar, Shraddha Shetty, Santosh Chhajed et Debjani Dasgupta. « <em>In silico</em> ; and <em>in vitro</em> ; study of benzanilide derivatives as potent anti-cancer agents ». Dans 6th International Electronic Conference on Medicinal Chemistry. Basel, Switzerland : MDPI, 2020. http://dx.doi.org/10.3390/ecmc2020-07699.

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