The Design Synthesis And Biological Evaluation Of Novel Antitumour Compounds

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Anticancer Agents

Author : Qiao-Hong Chen
Publisher : MDPI
ISBN 13 : 3036501401
Total Pages : 606 pages
Book Rating : 4.0/5 (365 download)

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Book Synopsis Anticancer Agents by : Qiao-Hong Chen

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.

Drug Design of Zinc-Enzyme Inhibitors

Author : Claudiu T. Supuran
Publisher : John Wiley & Sons
ISBN 13 : 9780470508152
Total Pages : 1040 pages
Book Rating : 4.5/5 (81 download)

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Book Synopsis Drug Design of Zinc-Enzyme Inhibitors by : Claudiu T. Supuran

Download or read book Drug Design of Zinc-Enzyme Inhibitors written by Claudiu T. Supuran and published by John Wiley & Sons. This book was released on 2009-10-22 with total page 1040 pages. Available in PDF, EPUB and Kindle. Book excerpt: Brings together functional and structural informationrelevant to the design of drugs targeting zinc enzymes The second most abundant transition element in living organisms, zinc spans all areas of metabolism, with zinc-containing proteins offering both established and potential drug targets. Drug Design of Zinc-Enzyme Inhibitors brings together functional and structural information relevant to these zinc-containing targets. With up-to-date overviews of the latest developments field, this unique and comprehensive text enables readers to understand zinc enzymes and evaluate them in a drug design context. With contributions from the leaders of today's research, Drug Design of Zinc-Enzyme Inhibitors covers such key topics as: Major drug targets like carbonic anhydrases, matrix metalloproteinases, bacterial proteases, angiotensin-converting enzyme, histone deacetylase, and APOBEC3G Roles of recently discovered zinc-containing isozymes in cancer, obesity, epilepsy, pain management, malaria, and other conditions Cross reactivity of zinc-enzyme inhibitors and activators The extensive use of X-ray crystallography and QSAR studies for understanding zinc-containing proteins Clinical applications An essential resource for the discovery and development of new drug molecules, Drug Design of Zinc-Enzyme Inhibitors gives researchers, professionals, students, and academics the foundation to understand and work with zinc enzyme inhibitors and activators.

Carbonic Anhydrase

Author : Claudiu T. Supuran
Publisher : CRC Press
ISBN 13 : 1134400152
Total Pages : 560 pages
Book Rating : 4.1/5 (344 download)

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Book Synopsis Carbonic Anhydrase by : Claudiu T. Supuran

Download or read book Carbonic Anhydrase written by Claudiu T. Supuran and published by CRC Press. This book was released on 2004-05-27 with total page 560 pages. Available in PDF, EPUB and Kindle. Book excerpt: Carbonic Anhydrase: Its Inhibitors and Activators provides a state-of-the-art overview of the latest developments and challenges in carbonic anhydrase research. Authors describe the mechanisms of action of specific inhibitors in relation to physiological function, and present previously unpublished research on CA activators. Written by a team of in

N-Heterocycles

Author : Keshav Lalit Ameta
Publisher : Springer Nature
ISBN 13 : 981190832X
Total Pages : 465 pages
Book Rating : 4.8/5 (119 download)

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Book Synopsis N-Heterocycles by : Keshav Lalit Ameta

Download or read book N-Heterocycles written by Keshav Lalit Ameta and published by Springer Nature. This book was released on 2022-04-23 with total page 465 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book presents an overview of the recent advancements for the synthesis of small- and medium-sized azaheterocycles, including pyrroles, indoles, pyrimidines, pyridines, pyrrolidines, imidazoles, pyrazoles, pyrazolines, lactams, and 1,2,3-triazoles, which are significant scaffolds for compounds with pharmaceutical uses. The book also discusses various properties and performance attributes of azaheterocycles including their bioactivity and synthetic strategies. Given the contents, the book will be a valuable reference for students, researchers, and professionals interested in organic synthesis and medicinal chemistry.

Anticancer Drug Development Guide

Author : Beverly A. Teicher
Publisher : Springer Science & Business Media
ISBN 13 : 1592597394
Total Pages : 514 pages
Book Rating : 4.5/5 (925 download)

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Book Synopsis Anticancer Drug Development Guide by : Beverly A. Teicher

Download or read book Anticancer Drug Development Guide written by Beverly A. Teicher and published by Springer Science & Business Media. This book was released on 2004-02-01 with total page 514 pages. Available in PDF, EPUB and Kindle. Book excerpt: This unique volume traces the critically important pathway by which a "molecule" becomes an "anticancer agent. " The recognition following World War I that the administration of toxic chemicals such as nitrogen mustards in a controlled manner could shrink malignant tumor masses for relatively substantial periods of time gave great impetus to the search for molecules that would be lethal to specific cancer cells. Weare still actively engaged in that search today. The question is how to discover these "anticancer" molecules. Anticancer Drug Development Guide: Preclinical Screening, Clinical Trials, and Approval, Second Edition describes the evolution to the present of preclinical screening methods. The National Cancer Institute's high-throughput, in vitro disease-specific screen with 60 or more human tumor cell lines is used to search for molecules with novel mechanisms of action or activity against specific phenotypes. The Human Tumor Colony-Forming Assay (HTCA) uses fresh tumor biopsies as sources of cells that more nearly resemble the human disease. There is no doubt that the greatest successes of traditional chemotherapy have been in the leukemias and lymphomas. Since the earliest widely used in vivo drug screening models were the murine L 1210 and P388 leukemias, the community came to assume that these murine tumor models were appropriate to the discovery of "antileukemia" agents, but that other tumor models would be needed to discover drugs active against solid tumors.

Boron-Based Compounds

Author : Evamarie Hey-Hawkins
Publisher : John Wiley & Sons
ISBN 13 : 1119275555
Total Pages : 490 pages
Book Rating : 4.1/5 (192 download)

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Book Synopsis Boron-Based Compounds by : Evamarie Hey-Hawkins

Download or read book Boron-Based Compounds written by Evamarie Hey-Hawkins and published by John Wiley & Sons. This book was released on 2018-07-23 with total page 490 pages. Available in PDF, EPUB and Kindle. Book excerpt: Noted experts review the current status of boron-containing drugs and materials for molecular medical diagnostics Boron-Based Compounds offers a summary of the present status and promotes the further development of new boron-containing drugs and advanced materials, mostly boron clusters, for molecular medical diagnostics. The knowledge accumulated during the past decades on the chemistry and biology of bioorganic and organometallic boron compounds laid the foundation for the emergence of a new area of study and application of boron compounds as lipophilic pharmacophores and modulators of biologically active molecules.This important text brings together in one comprehensive volume contributions from renowned experts in the field of medicinal chemistry of boron compounds. The authors cover a range of the most relevant topics including boron compounds as modulators of the bioactivity of biomolecules, boron clusters as pharmacophores or for drug delivery, boron compounds for boron neutron capture therapy (BNCT) and for diagnostics, as well as in silico molecular modeling of boron- and carborane-containing compounds in drug design. Authoritative and accessible, Boron-Based Compounds: Contains contributions from a panel of internationally renowned experts in the field Offers a concise summary of the current status of boron-containing drugs and materials used for molecular diagnostics Highlights the range and capacity of boron-based compounds in medical applications Includes information on boron neutron capture therapy and diagnostics Designed for academic and industrial scientists, this important resource offers the cutting-edge information needed to understand the current state of boron-containing drugs and materials for molecular medical diagnostics.

Anticancer Drugs

Author : Niamh M O’Boyle
Publisher : MDPI
ISBN 13 : 3039215868
Total Pages : 214 pages
Book Rating : 4.0/5 (392 download)

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Book Synopsis Anticancer Drugs by : Niamh M O’Boyle

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.

Chemistry and Applications of Benzimidazole and its Derivatives

Author : Maria Marinescu
Publisher : BoD – Books on Demand
ISBN 13 : 1789845521
Total Pages : 230 pages
Book Rating : 4.7/5 (898 download)

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Book Synopsis Chemistry and Applications of Benzimidazole and its Derivatives by : Maria Marinescu

Download or read book Chemistry and Applications of Benzimidazole and its Derivatives written by Maria Marinescu and published by BoD – Books on Demand. This book was released on 2019-10-02 with total page 230 pages. Available in PDF, EPUB and Kindle. Book excerpt: Finding new strategies for synthesizing benzimidazole derivatives and functionalizing the benzimidazole core has proved to be important due to the compound's various applications in medicine, chemistry, and other areas. The multitude of benzimidazole derivatives marketed as drugs has led to intensive research in the field for the discovery of new biologically active structures. The general applications of benzimidazole derivatives in materials chemistry, electronics, technology, dyes, pigments, and agriculture open up new research horizons. This book guides the rational design of benzimidazole derivatives synthesis with certain applications. Chapters cover such topics as therapeutic use of benzimidazole in conditions like diabetes, viruses, and parasitic diseases; X-ray crystal structure of selected benzimidazole derivatives; benzimidazole compounds for cancer therapy; and others.

Bioactive Heterocycles

Author : K. L. Ameta
Publisher : Nova Science Publishers
ISBN 13 : 9781622576364
Total Pages : 0 pages
Book Rating : 4.5/5 (763 download)

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Book Synopsis Bioactive Heterocycles by : K. L. Ameta

Download or read book Bioactive Heterocycles written by K. L. Ameta and published by Nova Science Publishers. This book was released on 2013 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book is a critical and lucid account of various synthetic methodologies and biological activities of different sized bioactive heterocyclic compounds. In effect, this book imparts a great deal of comprehensive reviews about the chemistry and biology of selected groups of heterocycles and natural products including important pharmaceuticals as well as agrochemical pesticides in one handy project. Besides, this compendious effort encompasses different methods of synthesis and biological evaluation of heterocyclic compounds. The main purpose of this book is to share the recent advances and scope of Bioactive Heterocycles for the future avenues in the field. It has specifically been designed by keeping in mind the wide interests of individuals engaged in the design and synthesis of biologically active heterocyclic compounds as well as research scientists in academia and industry. The authors expect this book to be a standard reference in Universities and industrial libraries.

The Molecular Targets and Therapeutic Uses of Curcumin in Health and Disease

Author : Bharat B. Aggarwal
Publisher : Springer Science & Business Media
ISBN 13 : 0387464018
Total Pages : 502 pages
Book Rating : 4.3/5 (874 download)

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Book Synopsis The Molecular Targets and Therapeutic Uses of Curcumin in Health and Disease by : Bharat B. Aggarwal

Download or read book The Molecular Targets and Therapeutic Uses of Curcumin in Health and Disease written by Bharat B. Aggarwal and published by Springer Science & Business Media. This book was released on 2007-08-06 with total page 502 pages. Available in PDF, EPUB and Kindle. Book excerpt: The medicinal uses of Curcumin (also called turmeric) have been known and described for more than 5000 years. A large body of recent research suggests that curcumin is potentially useful in the treatment of inflammatory diseases, through modulation of numerous molecular targets. This is the first monograph to focus on the potential use of curcumin in the treatment of cancer, diabetes, cardiovascular diseases, arthritis, Alzheimer’s, psoriasis and more.

Medicinal Chemistry of Anticancer Drugs

Author : Carmen Avendaño
Publisher : Elsevier
ISBN 13 : 0444626670
Total Pages : 767 pages
Book Rating : 4.4/5 (446 download)

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Book Synopsis Medicinal Chemistry of Anticancer Drugs by : Carmen Avendaño

Download or read book Medicinal Chemistry of Anticancer Drugs written by Carmen Avendaño and published by Elsevier. This book was released on 2015-06-11 with total page 767 pages. Available in PDF, EPUB and Kindle. Book excerpt: Medicinal Chemistry of Anticancer Drugs, Second Edition, provides an updated treatment from the point of view of medicinal chemistry and drug design, focusing on the mechanism of action of antitumor drugs from the molecular level, and on the relationship between chemical structure and chemical and biochemical reactivity of antitumor agents. Antitumor chemotherapy is a very active field of research, and a huge amount of information on the topic is generated every year. Cytotoxic chemotherapy is gradually being supplemented by a new generation of drugs that recognize specific targets on the surface or inside cancer cells, and resistance to antitumor drugs continues to be investigated. While these therapies are in their infancy, they hold promise of more effective therapies with fewer side effects. Although many books are available that deal with clinical aspects of cancer chemotherapy, this book provides a sorely needed update from the point of view of medicinal chemistry and drug design. - Presents information in a clear and concise way using a large number of figures - Historical background provides insights on how the process of drug discovery in the anticancer field has evolved - Extensive references to primary literature

Green Chemistry

Author : Hosam El-Din M. Saleh
Publisher : BoD – Books on Demand
ISBN 13 : 9535138472
Total Pages : 191 pages
Book Rating : 4.5/5 (351 download)

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Book Synopsis Green Chemistry by : Hosam El-Din M. Saleh

Download or read book Green Chemistry written by Hosam El-Din M. Saleh and published by BoD – Books on Demand. This book was released on 2018-02-28 with total page 191 pages. Available in PDF, EPUB and Kindle. Book excerpt: To an increasing extent, "green chemistry" is a new chemical and engineering approach of chemistry and engineering, dedicated to make manufacturing processes and our world as a whole more sustainable world with a growing tendency. "Green chemistry" approaches are based on ecofriendly technologies, aiming to reduce or eliminate the use of solvents, or render them efficient and safer. Moreover, this scientific field is devoted to reduction or elimination of prevailing environmental and health threats, which typically accompany chemical products and traditional processes. The present book "Green Chemistry" contains 9 selected chapters, starting with a general introductory chapter on "green chemistry," and covers many recent applications and developments based on the principles of "green chemistry." This book is considered the appropriate way to communicate the advances in green materials and their applications to the scientific community. Chemists, scientists and researchers from related areas, and undergraduates involved in environmental issues and interested in approaches to improve the quality of life could find an inspiring and effective guide by reading this book.

Chemical Epigenetics

Author : Antonello Mai
Publisher : Springer Nature
ISBN 13 : 3030429822
Total Pages : 569 pages
Book Rating : 4.0/5 (34 download)

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Book Synopsis Chemical Epigenetics by : Antonello Mai

Download or read book Chemical Epigenetics written by Antonello Mai and published by Springer Nature. This book was released on 2020-03-31 with total page 569 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book presents an authoritative review of the most significant findings about all the epigenetic targets (writers, readers, and erasers) and their implication in physiology and pathology. The book also covers the design, synthesis and biological validation of epigenetic chemical modulators, which can be useful as novel chemotherapeutic agents. Particular attention is given to the chemical mechanisms of action of these molecules and to the drug discovery prose which allows their identification. This book will appeal to students who want to know the extensive progresses made by epigenetics (targets and modulators) in the last years from the beginning, and to specialized scientists who need an instrument to quickly search and check historical and/or updated notices about epigenetics.

Molecular Structure Description

Author : Lemont Burwell Kier
Publisher :
ISBN 13 : 9780124065550
Total Pages : 286 pages
Book Rating : 4.0/5 (655 download)

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Book Synopsis Molecular Structure Description by : Lemont Burwell Kier

Download or read book Molecular Structure Description written by Lemont Burwell Kier and published by . This book was released on 1999 with total page 286 pages. Available in PDF, EPUB and Kindle. Book excerpt: The electrotopological state is a new approach to defining key structural features of a molecule in drug design. Combining both electronic and topological attributes, the E-State index facilitates the development of a structure - activity model, the definition of a pharmacophore, and the search through a database for similar or dissimilar compounds. The background for the method, the concept of the intrinsic state, and the E-State index as a function of the atom or group within the field of all atoms in a molecule are all described in this primer for a new structure paradigm. Software on the bundled CD-ROM allows the reader to compute and display the E-State indices for molecules, while examples in the book illustrate strategies that can be used in drug research.

Bioactive Heterocycles

Author :
Publisher :
ISBN 13 :
Total Pages : pages
Book Rating : 4.:/5 (123 download)

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Book Synopsis Bioactive Heterocycles by :

Download or read book Bioactive Heterocycles written by and published by . This book was released on with total page pages. Available in PDF, EPUB and Kindle. Book excerpt:

Tubulin-Binding Agents

Author : Teresa Carlomagno
Publisher : Springer
ISBN 13 : 3540690395
Total Pages : 339 pages
Book Rating : 4.5/5 (46 download)

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Book Synopsis Tubulin-Binding Agents by : Teresa Carlomagno

Download or read book Tubulin-Binding Agents written by Teresa Carlomagno and published by Springer. This book was released on 2009-05-28 with total page 339 pages. Available in PDF, EPUB and Kindle. Book excerpt: reviews. The SAR data are discussed in light of the structural information available for each agent. The second chapter focuses on the total synthesis of the marine sponge-derived polyketide discodermolide. A comprehensive survey of the synthetic chemistry efforts of several groups over a 14-year period is provided together with a compa- son of the different approaches. The third chapter describes a comprehensive study of the mechanisms of activity of microtubules stabilizing drugs. Thermodynamic, kinetic, structural and fu- tional data on microtubules stabilizing drugs are discussed in an interdisciplinary manner to generate a “time-resolved” picture of the interaction of the drugs with different tubulin forms. The fourth and fifth chapters review the efforts and achievements made in the characterization of the structure of the complexes of tubulin with microtubules stabilizing agents by NMR (Chapter 4) and EM (Chapter 5). Especially evident is the discrepancy of the results obtained for epothilones, where the two techniques deliver radically different structures of the bound drug. Both NMR and EM models are, however, able to explain a consistent set of SAR data. The authors of the two chapters discuss critically the advantages and limitations of each methodology.

Chemistry and Pharmacology of Anticancer Drugs

Author : David E. Thurston
Publisher : CRC Press
ISBN 13 : 1439853274
Total Pages : 619 pages
Book Rating : 4.4/5 (398 download)

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Book Synopsis Chemistry and Pharmacology of Anticancer Drugs by : David E. Thurston

Download or read book Chemistry and Pharmacology of Anticancer Drugs written by David E. Thurston and published by CRC Press. This book was released on 2021-03-17 with total page 619 pages. Available in PDF, EPUB and Kindle. Book excerpt: While drug therapies developed in the last 80 years have markedly improved treatment outcomes and the management of some types of cancers, the lack of effectiveness and side effects associated with the most common treatment types remain unacceptable. However, recent technological advances are leading to improved therapies based on targeting distinct biological pathways in cancer cells. Chemistry and Pharmacology of Anticancer Drugs is a comprehensive survey of all families of anticancer agents and therapeutic approaches currently in use or in advanced stages of clinical trials, including biological-based therapies. The book is unique in providing molecular structures for all anticancer agents, discussing them in terms of history of development, chemistry, mechanism of action, structure–function relationships, and pharmacology. It also provides relevant information on side effects, dosing, and formulation. The authors, renowned scientists in cancer research and drug discovery, also provide up-to-date information on the drug discovery process, including discussions of new research tools, tumor-targeting strategies, and fundamental concepts in the relatively new areas of precision medicine and chemoprevention. Chemistry and Pharmacology of Anticancer Drugs is an indispensable resource for cancer researchers, medicinal chemists and other biomedical scientists involved in the development of new anticancer therapies. Its breadth of coverage, clear explanations, and illustrations also make it suitable for undergraduate and postgraduate courses in medicine, pharmacy, nursing, dentistry, nutrition, the biomedical sciences, and related disciplines. Key Features: Summarizes the fundamental causes of cancer, modes of treatment, and strategies for cancer drug discovery Brings together a broad spectrum of information relating to the chemistry and pharmacology of all families of anticancer agents and therapies Includes up-to-date information on cutting-edge aspects of cancer treatments such as biomarkers, pharmacogenetics, and pharmacogenomics Features new chapters on the "Evolution of Anticancer Therapies", "Antibody-Based Therapies", and "Cancer Chemoprevention"