Download or read book Design Synthesis and Characterisation of Potential Anticancer Agents Based on Natural Products and Studies on Their Biological Effect written by Fredrick Obinna Ojike and published by . This book was released on 2018 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Anticancer Agents written by Qiao-Hong Chen and published by MDPI. This book was released on 2021-03-02 with total page 606 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book is a printed edition of the Special Issue entitled “Anticancer Agents: Design, Synthesis and Evaluation” that was published in Molecules. Two review articles and thirty research papers are included in the Special Issue. Three second-generation androgen receptor antagonists that have been approved by the U.S. FDA for the treatment of prostate cancer have been reviewed. Identification of mimics of protein partners as protein-protein interaction inhibitors via virtual screening has been summarized and discussed. Anticancer agents targeting various protein targets, including IGF-1R, Src, protein kinase, aromatase, HDAC, PARP, Toll-Like receptor, c-Met, PI3Kdelta, topoisomerase II, p53, and indoleamine 2,3-dioxygenase, have been explored. The analogs of three well-known tubulin-interacting natural products, paclitaxel, zampanolide, and colchicine, have been designed, synthesized, and evaluated. Several anticancer agents representing diverse chemical scaffolds were assessed in different kinds of cancer cell models. The capability of some anticancer agents to overcome the resistance to currently available drugs was also studied. In addition to looking into the in vitro ability of the anticancer agents to inhibit cancer cell proliferation, apoptosis, and cell cycle, in vivo antitumor efficacy in animal models and DFT were also investigated in some papers.
Download or read book Anticancer Agents from Natural Products Second Edition written by Gordon M. Cragg and published by CRC Press. This book was released on 2011-10-10 with total page 786 pages. Available in PDF, EPUB and Kindle. Book excerpt: The approach to drug discovery from natural sources has yielded many important new pharmaceuticals inaccessible by other routes. In many cases the isolated natural product may not be an effective drug for any of several reasons, but it nevertheless may become a drug through chemical modification or have a novel pharmacophore for future drug design. In summarizing the status of natural products as cancer chemotherapeutics, Anticancer Agents from Natural Products, Second Edition covers the: History of each covered drug—a discussion of its mechanism on action, medicinal chemistry, synthesis, and clinical applications Potential for novel drug discovery through the use of genome mining as well as future developments in anticancer drug discovery Important biosynthetic approaches to "unnatural" natural products Anticancer Agents from Natural Products, Second Edition discusses how complex target-oriented synthesis—enabled by historic advances in methodology—has enormously expanded the scope of the possible. This book covers the current clinically used anticancer agents that are either natural products or are clearly derived from natural product leads. It also reviews drug candidates currently in clinical development since many of these will be clinically used drugs in the future. Examples include the drugs etoposide and teniposide derived from the lead compound podophyllotoxin; numerous analogs derived from taxol; topotecan, derived from camptothecin; and the synthetic clinical candidates, E7389 and HTI-286, developed from the marine leads, halichondrin B and hemiasterlin.
Download or read book Anticancer Agents written by Qiao-Hong Chen and published by . This book was released on 2021 with total page 606 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book is a printed edition of the Special Issue entitled “Anticancer Agents: Design, Synthesis and Evaluation” that was published in Molecules. Two review articles and thirty research papers are included in the Special Issue. Three second-generation androgen receptor antagonists that have been approved by the U.S. FDA for the treatment of prostate cancer have been reviewed. Identification of mimics of protein partners as protein-protein interaction inhibitors via virtual screening has been summarized and discussed. Anticancer agents targeting various protein targets, including IGF-1R, Src, protein kinase, aromatase, HDAC, PARP, Toll-Like receptor, c-Met, PI3Kdelta, topoisomerase II, p53, and indoleamine 2,3-dioxygenase, have been explored. The analogs of three well-known tubulin-interacting natural products, paclitaxel, zampanolide, and colchicine, have been designed, synthesized, and evaluated. Several anticancer agents representing diverse chemical scaffolds were assessed in different kinds of cancer cell models. The capability of some anticancer agents to overcome the resistance to currently available drugs was also studied. In addition to looking into the in vitro ability of the anticancer agents to inhibit cancer cell proliferation, apoptosis, and cell cycle, in vivo antitumor efficacy in animal models and DFT were also investigated in some papers.
Download or read book Design Synthesis and Biological Evaluation of Nucleotide Prodrugs as Potential Anticancer Agents written by Rocco Valente and published by . This book was released on 2009 with total page 522 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Anticancer Agents from Natural Products written by Gordon M. Cragg and published by CRC Press. This book was released on 2005-06-13 with total page 610 pages. Available in PDF, EPUB and Kindle. Book excerpt: Plants, marine organisms, and microorganisms have evolved complex chemical defense and signaling systems that are designed to protect them from predators and provide other biological benefits. These organisms thus produce substances containing novel chemotypes that may have beneficial effects for humans. As collection methods improve and new screen
Download or read book Natural Products as Anticancer Agents written by Bimal Krishna Banik and published by Elsevier. This book was released on 2023-11-21 with total page 444 pages. Available in PDF, EPUB and Kindle. Book excerpt: Natural Products as Anticancer Agents introduces the different types of natural products that have been used for cancer treatment. Divided into four parts, covering anticancer agents derived from terrestrial plants, anticancer agents derived from the marine environment, and anticancer agents derived from microorganisms, as well as evaluation of new anticancer agents, each part includes discussion of the properties, synthesis/extraction, storage, mechanism of action, and usage of the molecules. Discussion of the future prospects in anticancer natural products—including several new trends and an indication of where research in this area is likely to go in the future—is also included. Assists in the identification of risk factors associated with the drug development process Includes process diagrams detailing the procedure for the isolation and purification of molecules Covers cost-effective green approaches in the development of anticancer drugs
Download or read book Computer assisted Design Synthesis and Biological Evaluation of New Aromatase Inhibitors as Potential Anticancer Agents written by Angelo Danilo Favia and published by . This book was released on 2005 with total page 122 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Design Synthesis and Biological Evaluation of Some Novel Nucleotide Prodrugs as Potential Anticancer Agents written by Costantino Congiatu and published by . This book was released on 2006 with total page 530 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Design Synthesis and Biological Evaluation of Novel Taxane based Anticancer Agents and Their Tumor Targeting Delivery written by Larisa Kuznetsova and published by . This book was released on 2005 with total page 584 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Design Synthesis and Biological Evaluation of Novel Taxane based Anticancer Agents and Their Applications to Tumor targeting Drug Delivery Systems written by Xianrui Zhao and published by . This book was released on 2009 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Design Synthesis and Biological Evaluation of Novel Tumor targeting Taxane based Anticancer Agents written by Jin Chen and published by . This book was released on 2006 with total page 373 pages. Available in PDF, EPUB and Kindle. Book excerpt: A novel series of the second-generation taxoid conjugates with o-3 polyunsaturated fatty acids (PUFA) such as docosahexanoic acid (DHA), linolenic acid (LNA) and linoleic acid (LA) has been successfully developed. The new conjugates, tested in vivo, exhibited strong activity against both resistant and sensitive colon and ovarian cancer xenografts. Two of the new conjugates (DHA-SB-T-1214 and DHA-SB-T-1213) caused the total regression of resistant and sensitive type cancers, respectively, with reduced side toxicity.
Download or read book Design Synthesis and Biological Evaluation of Dehydrozingerone Analogs as Anticancer Agents written by Jin Tatsuzaki and published by . This book was released on 2005 with total page 172 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Natural Products inspired Synthesis and Biological Evaluation of Bioactive Agents written by Jehad S. Almaliti and published by . This book was released on 2013 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt: Natural products are a prolific source of bioactive agents of diverse structure and varying biological activity. They are the single most productive source of lead molecules for developing clinically useful drugs for human disorders. Two different synthetic medicinal chemistry projects based on natural products were undertaken for my PhD research. The first research project focused on natural products-inspired synthesis of neuroprotective agents against H2O2-induced cell death. The second research project focused on the synthesis of novel largazole analogues targeting histone deacetylases to improve potency and isoform selectivity for treatment of cancer. Stroke is the fourth leading cause of death in the USA, where over 2000 new cases are diagnosed every day. Treatment options for stroke-related brain damage are very limited and there is an unmet need for effective neuroprotective agents to treat these conditions. Comparison of the structures of several classes of neuroprotective natural products such as limonoids and cardiac glycosides revealed the presence of a common structural motif which may account for their observed neuroprotective activity. Several natural product mimics that incorporate this shared structural motif were synthesized and were found to possess significant neuroprotective activity. These compounds enhanced cell viability against H2O2 induced oxidative stress or cell death in PC12 neuronal cells. The compounds were also found to enhance and modulate Na+/K+-ATPase activity of PC12 cells, which may suggest that the observed neuroprotective activity is mediated, at least partly, through interaction with Na+/K+-ATPase. Epigenetic regulation by altering gene expression without changing DNA sequences is a promising new strategy in developing anticancer agents. As histone deacetylases (HDAC) play an important role in gene expression, HDAC inhibitors have become an increasingly popular class of agents for targeting epigenetic regulation. Isoform and class-selective HDAC inhibitors are being developed to reduce the undesirable side effects resulting from non-selective HDAC inhibitory activity. Largazole is a potent and class I selective HDAC inhibitor recently isolated from a marine cyanobacterium of the genus Symploca. The depsipeptide ring of largazole constitutes the surface recognition cap group that interacts with the less conserved hydrophobic rim of the HDAC active site. In order to investigate the effect of the nature of this group on isoform and class selectivity, we have designed and synthesized largazole analogues with structural alterations in the depsipeptide ring (surface recognition cap group). In the designed analogues, the thiazole-thiazoline moiety of largazole is replaced with different aromatic and alkyl groups, to investigate the structure-activity relationship requirements. They include linear polyether group (analogue JA1), bi-pyridine group (analogue JA2), pyridine-methylamine group (analogue JA3), pyridine-benzylamine group (analogue JA4), pyridine-4-(trifluromethyl)benzylamine group (analogue JA5), and pyridine-4-methoxybenzylamine group (analogue JA6). The biological activities of the synthesized analogues JA1-JA6 are evaluated in the laboratory of Dr. Robert A. Casero, Jr. at the Johns Hopkins School of Medicine. The antiproliferative activity of analogues on HCT116 cells was evaluated using standard MTS reduction assay. The downstream effect of HDAC inhibition on global histone H3 acetylation has also been assayed using HCT116 cells. The isoform selectivity of the analogues is being determined using recombinant HDAC1, HDAC6, and HDAC8. The preliminary studies with analogue JA2 showed promising sub-nanomolar activity on many tumor cancer cell lines and is currently being further evaluated for synergistic activity with other clinically used anticancer agents. Additionally, analogues JA1-JA3 were found to be active at 10 æM in the 60 cell line human tumor screen at the National Cancer Institute (NCI) and they are currently being tested in the dose response assay.
Download or read book Design Synthesis and Biological Activity of Thioxanthenone Sulfoxides as Potential Bioreductive Anticancer Agents written by Hua-Zhong He and published by . This book was released on 2002 with total page 220 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Design Synthesis and Biological Evaluations of Novel Taxane based and Taxane free Anticancer Agents written by Xudong Geng and published by . This book was released on 2002 with total page 1608 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Design Synthesis and Biological Evaluation of Tumor targeting Taxane based Anticancer Agents and MDR Modulators written by Xinyuan Wu and published by . This book was released on 2003 with total page 754 pages. Available in PDF, EPUB and Kindle. Book excerpt:
