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 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.
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
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.
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.
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.
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.
Download or read book Doxorubicin written by Federico Arcamone and published by . This book was released on 1981 with total page 402 pages. Available in PDF, EPUB and Kindle. Book excerpt:
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.
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 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.
Download or read book Dark Remedy written by Trent Stephens and published by Basic Books. This book was released on 2009-04-27 with total page 244 pages. Available in PDF, EPUB and Kindle. Book excerpt: In this riveting medical detective story, Trent Stephens and Rock Brynner recount the history of thalidomide, from the epidemic of birth defects in the 1960's to the present day, as scientists work to create and test an alternative drug that captures thalidomide's curative properties without its cruel side effects. A parable about compassion-and the absence of it-Dark Remedy is a gripping account of thalidomide's extraordinary impact on the lives of individuals and nations over half a century.
Download or read book Carbonic Anhydrases and Metabolism written by Claudiu T. Supuran and published by MDPI. This book was released on 2019-04-08 with total page 184 pages. Available in PDF, EPUB and Kindle. Book excerpt: Carbonic anhydrases (CAs; EC 4.2.1.1) are metalloenzymes present in all kingdoms of life, as they equilibrate the reaction between three simple but essential chemical species: CO2, bicarbonate, and protons. Discovered more than 80 years ago, in 1933, these enzymes have been extensively investigated due to the biomedical application of their inhibitors, but also because they are an extraordinary example of convergent evolution, with seven genetically distinct CA families that evolved independently in Bacteria, Archaea, and Eukarya. CAs are also among the most efficient enzymes known in nature, due to the fact that the uncatalyzed hydration of CO2 is a very slow process and the physiological demands for its conversion to ionic, soluble species is very high. Inhibition of the CAs has pharmacological applications in many fields, such as antiglaucoma, anticonvulsant, antiobesity, and anticancer agents/diagnostic tools, but is also emerging for designing anti-infectives, i.e., antifungal, antibacterial, and antiprotozoan agents with a novel mechanism of action. Mitochondrial CAs are implicated in de novo lipogenesis, and thus selective inhibitors of such enzymes may be useful for the development of new antiobesity drugs. As tumor metabolism is diverse compared to that of normal cells, ultimately, relevant contributions on the role of the tumor-associated isoforms CA IX and XII in these phenomena have been published and the two isoforms have been validated as novel antitumor/antimetastatic drug targets, with antibodies and small-molecule inhibitors in various stages of clinical development. CAs also play a crucial role in other metabolic processes connected with urea biosynthesis, gluconeogenesis, and so on, since many carboxylation reactions catalyzed by acetyl-coenzyme A carboxylase or pyruvate carboxylase use bicarbonate, not CO2, as a substrate. In organisms other than mammals, e.g., plants, algae, and cyanobacteria, CAs are involved in photosynthesis, whereas in many parasites (fungi, protozoa), they are involved in the de novo synthesis of important metabolites (lipids, nucleic acids, etc.). The metabolic effects related to interference with CA activity, however, have been scarcely investigated. The present Special Issue of Metabolites aims to fill this gap by presenting the latest developments in the field of CAs and their role in metabolism.
Download or read book Heterocyclic Antitumor Antibiotics written by Moses Lee and published by . This book was released on 2006-05-22 with total page 280 pages. Available in PDF, EPUB and Kindle. Book excerpt: The series "Topics in Heterocyclic Chemistry" will present critical reviews on "Heterocyclic Compounds" within topic related volumes dealing with all aspects such as synthesis, reaction mechanisms, structure complexity, properties, reactivity, stability, fundamental and theoretical studies, biology, biomedical studies, pharmacological aspects, applications in material sciences etc. Metabolism will be also included which will provide information useful in designing pharmacologically active agents. Pathways involving destruction of heterocyclic ring will also be dealt with so that synthesis of specifically functionalized non-heterocyclic molecules can be designed. Overall scope is to cover topics dealing with most of the areas of current trends in heterocyclic chemistry which will suit to a larger heterocyclic community.
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.
Download or read book Drug Selectivity written by Norbert Handler and published by John Wiley & Sons. This book was released on 2018-02-27 with total page 538 pages. Available in PDF, EPUB and Kindle. Book excerpt: The book "Drug Selectivity - An Evolving Concept in Medicinal Chemistry" provides a current overview and comprehensive compilation for medicinal chemists that discusses the effects of aiming for multiple targets on the entire drug development process. The result is a broad survey of current and future strategies for drug selectivity in medicinal chemistry with theoretical but also practical aspects. Different strategies are presented and evaluated, such as various design approaches, merged multiple ligands, discovery technologies and a broad range of successful examples of unselective drugs taken from all major disease areas. With its wide-ranging view of an emerging new paradigm in drug development, this handbook is of prime importance for every medicinal and pharmaceutical chemist.
Download or read book Heterocycles written by B. P. Nandeshwarappa and published by . This book was released on 2020-06 with total page 202 pages. Available in PDF, EPUB and Kindle. Book excerpt:
