Volume 4 of Advances in Medicinal Chemistry is comprised of six chapters on a wide range of topics in medicinal chemistry, including molecular modeling, structure-based drug design, organic synthesis, peptide conformational analysis, biological assessment, structure-activity correlation, and lead optimization. Chapter 1 presents an account about amino acid-based peptide mimetics corresponding to b-turn, loop, helical motifs in proteins as a probe of ligand-receptor and ligand-enzyme molecular interactions. Chapter 2 addresses new facets of the medicinal chemistry of the important anticancer drug Taxol® (paclitaxel). Chapter 3 relates an account of the search for new drugs for the treatment of malaria based on the natural product artemisinin. Chapter 4 applies computational chemistry to the evaluation of compound libraries for biological testing. Chapter 5 describes the construction of a 3-dimensional molecular model of the human thrombin receptor, the first protease-activated G-protein coupled receptor (PAR-1), as a means to explore the intermolecular contacts involved in agonist peptide recognition. Finally, Chapter 6 describes the research conducted at Merck on inhibitors of farnesyl transferase as a potential treatment for human cancers.
Metal-based anticancer drugs are among the most successful therapeutic agents, as evidenced by the frequent prescription of selected platinum and arsenic compounds to patients. Metal-based Anticancer Agents covers the interdisciplinary world of inorganic drug discovery and development by introducing the most prominent compound classes based on different transition metals, discussing emerging concepts and enabling methods, as well as presenting key pre-clinical and clinical aspects. Recent progress on the unique features of next-generation targeted metal-based anticancer agents, including supramolecular coordination complexes used for both therapy and drug delivery, promise a bright future beyond the benefits of pure cytotoxic activity. With contributions from global leaders in the field, this book will serve as a useful reference to established researchers as well as a practical guide to those new to metallodrugs, and postgraduate students of medicinal chemistry and metallobiology.
Originally published by Bentham and now distributed by Elsevier, Recent Advances in Medicinal Chemistry, Volume 1 covers leading-edge research and recent developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, drug targets, and natural product research and structure-activity relationship studies. The fourteen updated reviews include unique experimental data and references, and each article highlights an important topic in current medicinal chemistry research. Topics covered include: aureolic acid group of anti-cancer antibiotics and non-steroidal anti-inflammatory drugs; aromatase inhibitors in adjuvant endocrine treatment of early-stage breast cancer in postmenopausal women; Rho GTPases and statins in targeting and developing therapies for tumors; and more. - Edited and written by leading experts in medicinal chemistry research - Reviews recent advances in the field, including the characterization of inorganic nanomaterials as therapeutic vehicles - Covers a variety of topical areas, such as HPLC and in the analysis of tricyclic antidepressants in biological samples, and tannins and their influence on health
This book is organized into 12 important chapters that focus on the progress made by metal-based drugs as anticancer, antibacterial, antiviral, anti-inflammatory, and anti-neurodegenerative agents, as well as highlights the application areas of newly discovered metallodrugs. It can prove beneficial for researchers, investigators and scientists whose work involves inorganic and coordination chemistry, medical science, pharmacy, biotechnology and biomedical engineering.
Advances in Anticancer Agents in Medicinal Chemistry is an exciting eBook series comprising a selection of updated articles previously published in the peer-reviewed journal Anti-Cancer Agents in Medicinal Chemistry. The second Volume of this eBook series gathers updated reviews on several classes of molecules exhibiting anticarcinogenic potential as well as some important targets for the development of novel anticancer drugs.
Advances in Medicinal Chemistry Research is a book addressed to undergraduate and postgraduate students, where recent advances in the discovery and development of effective agents against the most remarkable wide-reaching diseases are presented, divided into seven chapters. This first edition of Advances in Medicinal Chemistry Research offers insights into medicinal chemistry that arguably have the most significant impact on our lives than any other. It draws together research on therapeutic agents from natural, synthetic, and virtual screening sources as starting points for the design of drugs against obesity, multidrug-resistant bacteria, neglected tropical diseases, Alzheimer, and cancer. From the prediction of promising hits and identification of active compounds to the extraction of more complex molecules, this book explores a range of essential topics to support the development of novel, economical, and efficacious therapeutics for these diseases, which currently affect a billion people worldwide. Beginning with an overview of obesity, showing the current research landscape, the books shows the importance of natural and synthetic products as promising anti-obesity agents. Subsequently, the medicinal chemistry of modulation of bacterial resistance is presented, focusing on the MFS, RND, ABC, and MATE superfamilies. The book goes on to discuss such topics as antituberculosis, antileishmanial, and anti-hepatitis thiophene-containing compounds, under the medicinal chemistry point of view. Also, potent human glutaminyl cyclase inhibitors are deeply discussed and displayed as hopeful anti-Alzheimer's agents. The last three chapters are focused on the development of researches involving new anticancer agents, initializing with LBDD, SBDD, QSAR, and QM/MM methods applied to the identification of novel promising anticancer compounds. Moreover, IDO1 inhibitors are exhaustively explored and analyzed as a new promise for the immunotherapy of cancer. Finally, a great update on Eg5 kinesin inhibitors is provided, exploring different chemical classes of synthetic and natural compounds, including miscellanea as a new approach for Eg5 inhibition. Combining the expertise of researchers from around the world, this volume aims to support and encourage researches for the development of novel, safe, and active agents against lipase enzyme, bacteria, neglected tropical diseases, Alzheimer, and cancer. The clear narrative truly engages the reader, holding their attention right from the opening of a chapter, and maintaining interest and understanding as a chapter leads into more complex material. Advances in Medicinal Chemistry Research is a book that reviews ongoing developments and recent cutting-edge advances in medicinal chemistry of the most relevant diseases found nowadays, underlining how medicinal chemistry research continues to make significant contributions to the discovery and development of new therapeutic entities. Key Features â¢Chapters written by active specialists and leading experts deeply engaged in the research field of most deadly and limiting diseases for drug discovery. â¢Draws together cutting-edge research advances in medicinal chemistry focused at the obesity, multidrug-resistant microorganisms, Alzheimer, and cancer in a single volume. â¢Highlights the future potential of researches for the medicinal chemistry of most impactful diseases today. â¢Contents addressed to medicinal chemistry, biochemistry, biology, and pharmacy students, professors, and researchers.
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.
While drug therapies developed in the last 50 years have markedly improved the management of some types of cancers, treatment outcomes, and drug side-effects for the most common types remain unacceptable. However, recent technological advances are leading to improved therapies based on targeting distinct biological pathways in cancer cells.
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"
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
