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 a Series of Novel Aromatase Inhibitors Using a P450AROM Comparative Model written by Mohammad Reza Saberi and published by . This book was released on 2003 with total page 570 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Synthesis and Biological Evaluation of Potential Aromatase Inhibitors for Treatment of Hormone dependent Breast Cancer written by Masoud Ahmadi and published by . This book was released on 1989 with total page 470 pages. Available in PDF, EPUB and Kindle. Book excerpt:
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 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 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:
Download or read book Design Synthesis and Biological Evaluation of Novel Antiestrogens written by Rodrigo Mendoza Sánchez and published by . This book was released on 2013 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt: "Breast cancer is the most common form of cancer in women in the Western world and the second most fatal after lung cancer. Estrogens play a crucial role in normal breast development, but also contribute to mammary tumorigenesis. Estrogen signaling is mediated by intracellular estrogen receptors (ER[alpha] and ER[beta]), with ER[alpha] being a common target in breast cancer therapeutics. Two classes of competitive estrogen inhibitors have been investigated and proved to be useful for breast cancer treatment: full antiestrogens (FAE's) and selective estrogen receptor modulators (SERM's). A novel platform, FORECASTER, was developed in the Moitessier laboratory with the aim of integrating computational, medicinal and combinatorial chemistry. The successful validation of FORECASTER as a computer-aided drug design platform is described. In our quest for potent SERMs, this platform was used to build virtual combinatorial libraries and to filter and extract a highly diverse library from the NCI database. The virtual screening of a diverse library seeded with known active compounds followed by a search for analogs yielded a high enrichment factor. Moreover, the virtual screening of a designed virtual combinatorial library that included known actives resulted in a highly discriminative process. The laboratory of Dr. Sylvie Mader at University of Montreal showed that only FAE's induce a strong and fast SUMOylation of ER[alpha] in a variety of cell lines, strongly suggesting that SUMOylation is a general property related to full antiestrogenicity. A collaboration between the Gleason and Mader laboratories resulted in an SAR study of ER[alpha] ligands with different side chain lengths that revealed a specific side chain length of 15 to 19 atoms was necessary to differentiate SERM's from FAE's through the induction of SUMOylation. Histone deacetylase inhibitors (HDACi's) have emerged as a new and growing class of anticancer agents. Recent findings have shown that co-treatment of SERM's or FAE's with HDACi's can significantly decrease the growth of breast cancer cells. Inspired by the success of the vitamin D/HDACi hybrids developed within our group, and taking advantage of structural features of both kinds of molecules, we developed a new family of antiestrogen/HDACi hybrids. A first generation set of hybrids were designed by replacing the tertiary amide of FAE ICI-164,384 with three different zinc binding groups: hydroxamic acid, o-aminoanilide and N-butylhydroxamate. Both the hydroxamic acid and the o-aminoanilide hybrids displayed both antiestrogenic and HDAC inhibitory activities whereas N-butylhydroxamate hybrid displayed antiestrogenic activity but a poor HDAC inhibition profile. All hybrids inhibited MCF-7 cell proliferation and validated the proof of concept regarding the formation of this class of hybrids. However, none of the hybrids showed an improved profile compared to known antiestrogens or HDACi's. A second generation set of hybrids exploiting the same zinc binding groups with SERM- and FAE-like side chains were developed in an effort to balance the activity of our hybrids. Hydroxamic acids showed a consistent inhibition of HDAC's while displaying poor antiestrogenic activity in most cases. Ortho-amino anilides showed modest HDAC inhibition activity and only aliphatic-based o-amino-anilides behaved as antiestrogens. N-Butyl-hydroxamates showed a reduced potency to inhibit HDAC's compared to their hydroxamic acid counterparts but retained antiestrogenic behaviour. Overall, our second-generation hybrids did not show equal or improved HDAC inhibition and antiestrogenic activities relative to known antiestrogens and HDACi's. " --
Download or read book Exploring QSAR Fundamentals and applications in chemistry and biology written by Corwin Hansch and published by . This book was released on 1995 with total page 584 pages. Available in PDF, EPUB and Kindle. Book excerpt: [Volume 2]: This volume contains comprehensive tables of physicochemical parameters (substituent constants and octanol-water log P values) that are necessary for Quantitative Structure-Activity Relationships (QSAR) and qualitative SAR. Almost all of the world's environmental protection agencies require log P values for new industrial chemicals. These values were collected over 25 years by two of the most renowned researchers in the field.
Download or read book Phytochemicals written by Venketeshwer Rao and published by BoD – Books on Demand. This book was released on 2015-09-30 with total page 351 pages. Available in PDF, EPUB and Kindle. Book excerpt: Global dietary recommendations emphasize the consumption of plant-based foods for the prevention and management of chronic diseases. Plants contain many biologically active compounds referred to as phytochemicals or functional ingredients. These compounds play an important role in human health. Prior to establishing the safety and health benefits of these compounds, they must first be isolated, purified, and their physico-chemical properties established. Once identified, their mechanisms of actions are studied. The chapters are arranged in the order from isolation, purification and identification to in vivo and clinical studies, there by covering not only the analytical procedures used but also their nutraceutical and therapeutic properties.
Download or read book Anticancer Drugs written by Niamh M O’Boyle and published by MDPI. This book was released on 2019-10-11 with total page 214 pages. Available in PDF, EPUB and Kindle. Book excerpt: The past decades have seen major developments in the understanding of the cellular and molecular biology of cancer. Significant progress has been achieved regarding long-term survival for the patients of many cancers with the use of tamoxifen for treatment of breast cancer, treatment of chronic myeloid leukaemia with imatinib, and the success of biological drugs. The transition from cytotoxic chemotherapy to targeted cancer drug discovery and development has resulted in an increasing selection of tools available to oncologists. In this Special Issue of Pharmaceuticals, we highlight the opportunities and challenges in the discovery and design of innovative cancer therapies, novel small-molecule cancer drugs and antibody–drug conjugates, with articles covering a variety of anticancer therapies and potential relevant disease states and applications. Significant efforts are being made to develop and improve cancer treatments and to translate basic research findings into clinical use, resulting in improvements in survival rates and quality of life for cancer patients. We demonstrate the possibilities and scope for future research in these areas and also highlight the challenges faced by scientists in the area of anticancer drug development leading to improved targeted treatments and better survival rates for cancer patients.
Download or read book Research Awards Index written by and published by . This book was released on 1987 with total page 852 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Cooperative Catalysis written by René Peters and published by John Wiley & Sons. This book was released on 2015-04-27 with total page 452 pages. Available in PDF, EPUB and Kindle. Book excerpt: Written by experts in the field, this is a much-needed overview of the rapidly emerging field of cooperative catalysis. The authors focus on the design and development of novel high-performance catalysts for applications in organic synthesis (particularly asymmetric synthesis), covering a broad range of topics, from the latest progress in Lewis acid / Br?nsted base catalysis to e.g. metal-assisted organo catalysis, cooperative metal/enzyme catalysis, and cooperative catalysis in polymerization reactions and on solid surfaces. The chapters are classified according to the type of cooperating activating groups, and describe in detail the different strategies of cooperative activation, highlighting their respective advantages and pitfalls. As a result, readers will learn about the different concepts of cooperative catalysis, their corresponding modes of operation and their applications, thus helping to find a solution to a specific synthetic catalysis problem.
Download or read book Annual Review of Pharmacology and Toxicology written by Cho and published by . This book was released on 2000-04 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book American Doctoral Dissertations written by and published by . This book was released on 1995 with total page 896 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Molecular Interaction Fields written by Gabriele Cruciani and published by John Wiley & Sons. This book was released on 2006-05-12 with total page 328 pages. Available in PDF, EPUB and Kindle. Book excerpt: This unique reference source, edited by the world's most respected expert on molecular interaction field software, covers all relevant principles of the GRID force field and its applications in medicinal chemistry. Entire chapters on 3D-QSAR, pharmacophore searches, docking studies, metabolism predictions and protein selectivity studies, among others, offer a concise overview of this emerging field. As an added bonus, this handbook includes a CD-ROM with the latest commercial versions of the GRID program and related software.
Download or read book Multi Drug Resistance in Cancer written by Jun Zhou and published by Humana Press. This book was released on 2012-08-09 with total page 492 pages. Available in PDF, EPUB and Kindle. Book excerpt: Chemotherapy is one of the major treatment options for cancer patients; however, the efficacy of chemotherapeutic management of cancer is severely limited by multidrug resistance, in that cancer cells become simultaneously resistant to many structurally and mechanistically unrelated drugs. In the past three decades, a number of mechanisms by which cancer cells acquire multidrug resistance have been discovered. In addition, the development of agents or strategies to overcome resistance has been the subject of intense study. This book contains comprehensive and up-to-date reviews of multidrug resistance mechanisms, from over-expression of ATP-binding cassette drug transporters such as P-glycoprotein, multidrug resistance-associated proteins, and breast cancer resistance p- tein to the drug ratio-dependent antagonism and the paradigm of cancer stem cells. The book also includes strategies to overcome multidrug resistance, from the development of compounds that inhibit drug transporter function to the modulation of transporter expression. In addition, this book contains techniques for the detection and imaging of drug transporters, methods for the investigation of drug resistance in animal models, and strategies to evaluate the efficacy of resistance reversal agents. The book intends to provide a state-of-the-art collection of reviews and methods for both basic and clinician investigators who are interested in cancer multidrug resistance mechanisms and reversal strategies. Tianjin, China Jun Zhou v Contents Preface. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . v Contributors. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . ix 1 Multidrug Resistance in Cancer . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 1 Bruce C. Baguley 2 Multidrug Resistance in Oncology and Beyond: From Imaging of Drug Efflux Pumps to Cellular Drug Targets . . . . . . . . . . . . . . . . . . . . . . . . . .
Download or read book Cumulated Index Medicus written by and published by . This book was released on 2000 with total page 1844 pages. Available in PDF, EPUB and Kindle. Book excerpt:
