Download or read book Key Heterocycle Cores for Designing Multitargeting Molecules written by Om Silakari and published by Elsevier. This book was released on 2018-06-11 with total page 438 pages. Available in PDF, EPUB and Kindle. Book excerpt: Key Heterocycle Cores for Designing Multitargeting Molecules provides a helpful overview of current developments in the field. Following a detailed introduction to the manipulation of heterocycle cores for the development of dual or multitargeting molecules, the book goes on to describe specific examples of such developments, focusing on compounds such as Benzimidazole, Acridine, Flavones, Thiazolidinedione and Oxazoline. Drawing on the latest developments in the field, this volume provides a valuable guide to current approaches in the design and development of molecules capable of acting on multiple targets. Adapting the heterocyclic core of a single-target molecule can facilitate its development into an agent capable of acting on multiple targets. Such multi-targeting drugs have the potential to become essential components in the design of novel, holistic treatment plans for complex diseases, making the design of such active agents an increasingly important area of research. - Emphasizes the chemical development of heterocyclic nuclei, from single to multitargeting molecules - Provides chapter-by-chapter coverage of the key heterocyclic compounds used in synthesizing multitargeting agents - Outlines current trends and future developments in multitarget molecule design for the treatment of various diseases

Download or read book Vicinal Diaryl Substituted Heterocycles written by M. R. Yadav and published by Elsevier. This book was released on 2018-03-14 with total page 432 pages. Available in PDF, EPUB and Kindle. Book excerpt: Vicinal Diaryl-Substituted Heterocycles: A Gold Mine for the Discovery of Novel Therapeutic Agents draws together all of the key information about these compounds in one place for the first time. Following an informative overview of the importance of these structures to the discovery of potential therapeutic agents, the text goes on to outline the main compound types, with each chapter focusing on the activities of a different structure. Designed to support researchers by consolidating this important information in a single, practical guide, the authors hope to encourage further advancement and development in the discovery of novel therapeutic agents. As flexible building blocks for the production of novel compounds, vicinal diaryl-substituted heterocycles are a rich source of leads for the development of new drugs. Their adaptability means that they can be used to produce structures with a broad range of attractive characteristics, and a large number of vicinal diaryl-substituted heterocyclic compounds have already been synthesized and investigated by medicinal chemists as promising lead molecules. - Collects together details of the key vicinal diaryl-substituted heterocyclic compounds in one place for the first time - Highlights biological activities and SAR of derivatives - Structured practically for ease of navigation between different derivatives

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 Anticancer Agents written by Bimal Krishna Banik and published by Walter de Gruyter GmbH & Co KG. This book was released on 2022-06-21 with total page 1185 pages. Available in PDF, EPUB and Kindle. Book excerpt: Cancer is an incredibly diverse and difficult disease to treat, and even after decades of research there is no definitive cure. Therefore, it is highly crucial to search for novel and new organic molecules with high potency, low toxicity, and low mutagenicity with selective anticancer properties that are able to overcome frequently developed resistance to available drugs. Heterocyclic anticancer agents are an important class of drugs for cancer therapies. This book explores different heterocycles and their use as anticancer therapies. Topics covered include different heterocyclic derivatives, the impact of heterocycles on anticancer agent development, and naturally occurring heterocycles.

Download or read book Nanotechnology Based Precision Tools for the Detection and Treatment of Cancer written by Chad A. Mirkin and published by Springer. This book was released on 2015-04-20 with total page 327 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book discusses emerging nanotechnology-based tools that have the potential to dramatically impact cancer research, diagnostics, and treatment. Cancer is a complex, devastating, and debilitating disease and, although much progress has been made, novel, more effective diagnostic and treatment options are still needed, especially for advanced cancers. The ultimate goal is to detect cancer early and non-invasively and to provide efficacious and targeted precision treatments that cause fewer harmful side effects. This book explains how nanotechnology can exploit the size-, shape-, and composition-dependent properties of nanomaterials to provide novel tools for precision cancer medicine. It will be of interest to researchers and professionals working in the fields of chemistry, biology, materials science and engineering, and medicine who want to learn more about this fascinating and fast-paced area of research.

Download or read book Heterocyclic Scaffolds I written by Bimal K. Banik and published by Springer. This book was released on 2010-06-01 with total page 386 pages. Available in PDF, EPUB and Kindle. Book excerpt: Contents: B. Alcaide ∙ P. Almendros: Novel Aspects on the Preparation of Spirocyclic and Fused Unsual β-Lactams.- S.S. Bari ∙ A. Bhalla: Spirocyclic β-Lactams: Synthesis and Biological Evaluation of Novel Heterocycles.- L. Troisi ∙ C. Granito ∙ E. Pindinelli: Novel and Recent Synthesis and Applications of β-Lactams.- C. Palomo ∙ M. Oiarbide: β-Lactams Ring Opening: A Useful Entry to Amino Acids and Relevant Nitrogen-Containing Compounds.- B. Mandal ∙ P. Ghosh ∙ B. Basu: Recent Approaches Towards Solid Phase Synthesis of β-Lactams.- A.Arrieta ∙ B. Lecea ∙ F.P. Cossio: Computational Studies on the Synthesis of β-Lactams Via [ 2+2] Thermal Cycloadditions.- B. K. Banik ∙ I. Banik ∙ F. F. Becker: Novel Anticancer β-Lactams

Download or read book Key Heterocyclic Cores for Smart Anticancer Drug Design Part II written by Rajesh Kumar Singh and published by Bentham Science Publishers. This book was released on 2022-09-02 with total page 231 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book provides an update on heterocyclic compounds that serve as key components of anti-cancer agents administered in pre-clinical settings. Many of the compounds highlighted in the book are being actively investigated for the bioactive properties against a range of cancer cell lines. There is potential for heterocyclic compounds to design agents that can target specific molecules to treat different types of cancers. Chapters are contributed by experts in pharmaceutical chemistry and are written to give a general overview of the topic to readers involved in all levels of research and decision-making in pharmaceutical chemistry and anti-cancer drug design. Part 2 of the book set covers these topics: - Anticancer targets for heterocyclic lead compounds - Coumarin hybrids for cancer treatments - Progress in nitrogen and sulphur-based heterocyclic compounds for their anticancer activity - Imidazole as an anticancer heterocyclic ring - Morpholine for profiling anticancer lead compounds - Natural products as anticancer agents

Download or read book Novel Apoptotic Regulators in Carcinogenesis written by George G. Chen and published by Springer Science & Business Media. This book was released on 2012-08-28 with total page 305 pages. Available in PDF, EPUB and Kindle. Book excerpt: Our recent understanding of the cellular and molecular defects and the regulation of the apoptotic signalling pathways has resulted in rationally designed anticancer strategies and the development of novel agents that regulates apoptosis. A comprehensive review of all apoptotic-related anticancer therapies is not the purpose of this book. However, in the volume of this book with 11 chapters, we have described a number of novel apoptotic regulators that have shown promising value and also great feasibility for cancer treatment. These novel agents either occur naturally or are chemically synthesized. While we are excited about the discovery and development of these novel apoptotic regulators as potential anticancer agents, a degree of caution should be always borne in mind when interpreting the success of preclinical pro-apoptotic candidates since potential problems inevitably lie ahead. These problems usually include target specificity, unanticipated toxicity, compound stability, formulation issues, pharmacokinetic and pharmacodynamic profiles. Nevertheless, we believe that this collection of 11 chapters by established leaders in the area of apoptosis will be of great interest to not only academics working in the field of cancer research and apoptosis but also pharmaceutical and pharmacological industries that . We are looking forward to the further development to push these potential agents toward clinical stage.

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 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 Current Molecular Targets of Heterocyclic Compounds for Cancer Therapy written by Vivek Asati and published by Elsevier. This book was released on 2024-04-10 with total page 504 pages. Available in PDF, EPUB and Kindle. Book excerpt: Current Molecular Targets of Heterocyclic Compounds for Cancer Therapy discusses recently developed treatments based on molecular targets which are genetically altered in cancer cells and are essential for tumor development and survival. Considerable research effort has been devoted to the development of targeted drugs that inhibit the action of pathogenic kinases, and clinical studies performed so far have validated the positive effects of kinase inhibitors for cancer treatment. Each chapter discusses a molecular target, such as ALK2, ATR, CK, Src-Abl, EGFR, Fyn-Blk-Lyn, IGFs, and PAK1. The book's chapters are written by experts who actively work on the targets to help readers fully understand how they can be used. This is a valuable resource for cancer researchers, oncologists, graduate students and members of the biomedical field who are interested in the potential of novel cancer therapies based on molecular targets. - Discusses recently discovered molecular targets for cancer therapy - Brings updated literature of heterocyclic compounds, an important construction motif for the development of new anticancer drugs - Encompasses comprehensive compilation of recently introduced anticancer drugs in the market and their health outcomes and pharmacoeconomics

Download or read book Quinazolinone and Quinazoline Derivatives written by Ali Gamal Al-kaf and published by BoD – Books on Demand. This book was released on 2020-05-06 with total page 128 pages. Available in PDF, EPUB and Kindle. Book excerpt: One of the problems with modern public health is target searching for new highly effective medicinal preparations. Among those medicinal preparations are the natural and synthetic origins of quinazolinone-4 derivatives. Quinazolinone derivatives are reported to be physiologically and pharmacologically active. They also exhibit a wide range of activities such as anticonvulsant, antiinflammatory, antifungal, antimalarial, and sedative properties. Some of these compounds are identified as drugs used as diuretics, vasodilators, and antihypertensive agents. Moreover, sulfonamide derivatives have been widely used as bacteriostatic agents. Prompted by the above-mentioned facts and in conjunction with our ongoing program on the utility of readily obtainable starting material for the synthesis of heterocyclic systems of biological interest, we have decided to synthesize a series of quinazolinone derivatives having sulfonamide moiety with a potentially wide spectrum of biological responses.

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:

Download or read book Fundamentals of Inflammation written by Charles N. Serhan and published by Cambridge University Press. This book was released on 2010-04-26 with total page 489 pages. Available in PDF, EPUB and Kindle. Book excerpt: The acute inflammatory response is the body's first system of alarm signals that are directed toward containment and elimination of microbial invaders. Uncontrolled inflammation has emerged as a pathophysiologic basis for many widely occurring diseases in the general population that were not initially known to be linked to the inflammatory response, including cardiovascular disease, asthma, arthritis, and cancer. To better manage treatment, diagnosis, and prevention of these wide-ranging diseases, multidisciplinary research efforts are underway in both academic and industry settings. This book provides an introduction to the cell types, chemical mediators, and general mechanisms of the host's first response to invasion. World-class experts from institutions around the world have written chapters for this introductory text. The text is presented as an introductory springboard for graduate students, medical scientists, and researchers from other disciplines wishing to gain an appreciation and working knowledge of current cellular and molecular mechanisms fundamental to inflammation.

Download or read book Advances in Metallodrugs written by Shahid Ul Islam and published by John Wiley & Sons. This book was released on 2020-07-08 with total page 432 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Download or read book Advances in Novel Natural Product Pesticides written by Pei Li and published by Frontiers Media SA. This book was released on 2022-11-28 with total page 219 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Download or read book Medicinal Organometallic Chemistry written by Gérard Jaouen and published by Springer Science & Business Media. This book was released on 2010-09-14 with total page 305 pages. Available in PDF, EPUB and Kindle. Book excerpt: Contents: Gérard Jaouen, Nils Metzler-Nolte : Introduction ; Stéphane GIBAUD and Gérard JAOUEN: Arsenic - based drugs: from Fowler’s solution to modern anticancer chemotherapy; Ana M. Pizarro, Abraha Habtemariam and Peter J. Sadler : Activation Mechanisms for Organometallic Anticancer Complexes; Angela Casini, Christian G. Hartinger, Alexey A. Nazarov, Paul J. Dyson : Organometallic antitumour agents with alternative modes of action; Elizabeth A. Hillard, Anne Vessières, Gerard Jaouen : Ferrocene functionalized endocrine modulators for the treatment of cancer; Megan Hogan and Matthias Tacke : Titanocenes – Cytotoxic and Anti-Angiogenic Chemotherapy Against Advanced Renal-Cell Cancer; Seann P. Mulcahy and Eric Meggers : Organometallics as Structural Scaffolds for Enzyme Inhibitor Design; Christophe Biot and Daniel Dive : Bioorganometallic Chemistry and Malaria; Nils Metzler-Nolte : Biomedical applications of organometal-peptide conjugates; Roger Alberto : Organometallic Radiopharmaceuticals; Brian E. Mann : Carbon Monoxide – an essential signaling molecule.