The Design Synthesis And Biological Evaluation Of Novel Small Molecule Hdac Inhibitors

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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.

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.

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.

Practical Medicinal Chemistry with Macrocycles

Author : Eric Marsault
Publisher : John Wiley & Sons
ISBN 13 : 1119092566
Total Pages : 617 pages
Book Rating : 4.1/5 (19 download)

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Book Synopsis Practical Medicinal Chemistry with Macrocycles by : Eric Marsault

Download or read book Practical Medicinal Chemistry with Macrocycles written by Eric Marsault and published by John Wiley & Sons. This book was released on 2017-09-12 with total page 617 pages. Available in PDF, EPUB and Kindle. Book excerpt: Including case studies of macrocyclic marketed drugs and macrocycles in drug development, this book helps medicinal chemists deal with the synthetic and conceptual challenges of macrocycles in drug discovery efforts. Provides needed background to build a program in macrocycle drug discovery –design criteria, macrocycle profiles, applications, and limitations Features chapters contributed from leading international figures involved in macrocyclic drug discovery efforts Covers design criteria, typical profile of current macrocycles, applications, and limitations

Structural Biology in Drug Discovery

Author : Jean-Paul Renaud
Publisher : John Wiley & Sons
ISBN 13 : 1118900502
Total Pages : 1437 pages
Book Rating : 4.1/5 (189 download)

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Book Synopsis Structural Biology in Drug Discovery by : Jean-Paul Renaud

Download or read book Structural Biology in Drug Discovery written by Jean-Paul Renaud and published by John Wiley & Sons. This book was released on 2020-01-09 with total page 1437 pages. Available in PDF, EPUB and Kindle. Book excerpt: With the most comprehensive and up-to-date overview of structure-based drug discovery covering both experimental and computational approaches, Structural Biology in Drug Discovery: Methods, Techniques, and Practices describes principles, methods, applications, and emerging paradigms of structural biology as a tool for more efficient drug development. Coverage includes successful examples, academic and industry insights, novel concepts, and advances in a rapidly evolving field. The combined chapters, by authors writing from the frontlines of structural biology and drug discovery, give readers a valuable reference and resource that: Presents the benefits, limitations, and potentiality of major techniques in the field such as X-ray crystallography, NMR, neutron crystallography, cryo-EM, mass spectrometry and other biophysical techniques, and computational structural biology Includes detailed chapters on druggability, allostery, complementary use of thermodynamic and kinetic information, and powerful approaches such as structural chemogenomics and fragment-based drug design Emphasizes the need for the in-depth biophysical characterization of protein targets as well as of therapeutic proteins, and for a thorough quality assessment of experimental structures Illustrates advances in the field of established therapeutic targets like kinases, serine proteinases, GPCRs, and epigenetic proteins, and of more challenging ones like protein-protein interactions and intrinsically disordered proteins

The Cystic Fibrosis Transmembrane Conductance Regulator

Author : Kevin L. Kirk
Publisher : Springer Science & Business Media
ISBN 13 : 9780306478376
Total Pages : 236 pages
Book Rating : 4.4/5 (783 download)

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Book Synopsis The Cystic Fibrosis Transmembrane Conductance Regulator by : Kevin L. Kirk

Download or read book The Cystic Fibrosis Transmembrane Conductance Regulator written by Kevin L. Kirk and published by Springer Science & Business Media. This book was released on 2003-10-31 with total page 236 pages. Available in PDF, EPUB and Kindle. Book excerpt: The CFTR chloride channel is one of the most well studied transport proteins in biology. Yet there remain many mysteries about the functional properties and biological roles of this ABC transporter. The Cystic Fibrosis Transmembrane Conductance Regulator addresses a select series of `hot' topics that relate to the function of CFTR, and the links between CFTR dysfunction and human disease (i.e., cystic fibrosis). The timeliness of these topics distinguishes this collection from previous volumes of this type. Given the general interest in CFTR, this collection will appeal to a broad readership with interests in CFTR, cystic fibrosis, ion channels and ABC transporters.

Metal-based Anticancer Agents

Author : Angela Casini
Publisher : Royal Society of Chemistry
ISBN 13 : 1788017676
Total Pages : 370 pages
Book Rating : 4.7/5 (88 download)

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Book Synopsis Metal-based Anticancer Agents by : Angela Casini

Download or read book Metal-based Anticancer Agents written by Angela Casini and published by Royal Society of Chemistry. This book was released on 2019-04-05 with total page 370 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Proteomics for Biological Discovery

Author : Timothy D. Veenstra
Publisher : John Wiley & Sons
ISBN 13 : 0470007737
Total Pages : 361 pages
Book Rating : 4.4/5 (7 download)

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Book Synopsis Proteomics for Biological Discovery by : Timothy D. Veenstra

Download or read book Proteomics for Biological Discovery written by Timothy D. Veenstra and published by John Wiley & Sons. This book was released on 2006-06-12 with total page 361 pages. Available in PDF, EPUB and Kindle. Book excerpt: Written by recognized experts in the study of proteins, Proteomics for Biological Discovery begins by discussing the emergence of proteomics from genome sequencing projects and a summary of potential answers to be gained from proteome-level research. The tools of proteomics, from conventional to novel techniques, are then dealt with in terms of underlying concepts, limitations and future directions. An invaluable source of information, this title also provides a thorough overview of the current developments in post-translational modification studies, structural proteomics, biochemical proteomics, microfabrication, applied proteomics, and bioinformatics relevant to proteomics. Presents a comprehensive and coherent review of the major issues faced in terms of technology development, bioinformatics, strategic approaches, and applications Chapters offer a rigorous overview with summary of limitations, emerging approaches, questions, and realistic future industry and basic science applications Discusses higher level integrative aspects, including technical challenges and applications for drug discovery Accessible to the novice while providing experienced investigators essential information Proteomics for Biological Discovery is an essential resource for students, postdoctoral fellows, and researchers across all fields of biomedical research, including biochemistry, protein chemistry, molecular genetics, cell/developmental biology, and bioinformatics.

PET Chemistry

Author : P.A. Schubiger
Publisher : Springer Science & Business Media
ISBN 13 : 3540495274
Total Pages : 348 pages
Book Rating : 4.5/5 (44 download)

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Book Synopsis PET Chemistry by : P.A. Schubiger

Download or read book PET Chemistry written by P.A. Schubiger and published by Springer Science & Business Media. This book was released on 2007-01-19 with total page 348 pages. Available in PDF, EPUB and Kindle. Book excerpt: Personalized medicine employing patient-based tailor-made therapeutic drugs is taking over treatment paradigms in a variety of ?elds in oncology and the central nervous system. The success of such therapies is mainly dependent on ef?cacious therapeutic drugs and a selective imaging probe for identi?cation of potential responders as well as therapy monitoring for an early bene?t assessment. Molecular imaging (MI) is based on the selective and speci?c interaction of a molecular probe with a biological target which is visualized through nuclear, magnetic resonance, near infrared or other methods. Therefore it is the method of choice for patient selection and therapy monitoring as well as for speci?c e- point monitoring in modern drug development. PET (positron emitting tomography), a nuclear medical imaging modality, is ideally suited to produce three-dimensional images of various targets or processes. The rapidly increasing demand for highly selective probes for MI strongly pushes the development of new PET tracers and PET chemistry. ‘PET chemistry’ can be de?ned as the study of positron-emitting compounds regarding their synthesis, structure, composition, reactivity, nuclear properties and processes and their properties in natural and - natural environments. In practice PET chemistry is strongly in?uenced by the unique properties of the radioisotopes used (e. g. , half-life, che- cal reactivity, etc. ) and integrates scienti?c aspects of nuclear-, organic-, inorganic- and biochemistry.

Innovations for Next-Generation Antibody-Drug Conjugates

Author : Marc Damelin
Publisher : Springer
ISBN 13 : 3319781545
Total Pages : 358 pages
Book Rating : 4.3/5 (197 download)

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Book Synopsis Innovations for Next-Generation Antibody-Drug Conjugates by : Marc Damelin

Download or read book Innovations for Next-Generation Antibody-Drug Conjugates written by Marc Damelin and published by Springer. This book was released on 2018-05-29 with total page 358 pages. Available in PDF, EPUB and Kindle. Book excerpt: Antibody-drug conjugates (ADCs) stand at the verge of a transformation. Scores of clinical programs have yielded only a few regulatory approvals, but a wave of technological innovation now empowers us to overcome past technical challenges. This volume focuses on the next generation of ADCs and the innovations that will enable them. The book inspires the future by integrating the field’s history with novel strategies and cutting-edge technologies. While the book primarily addresses ADCs for solid tumors, the last chapter explores the emerging interest in using ADCs to treat other diseases. The therapeutic rationale of ADCs is strong: to direct small molecules to the desired site of action (and away from normal tissues) by conjugation to antibodies or other targeting moieties. However, the combination of small and large molecules imposes deep complexity to lead optimization, pharmacokinetics, toxicology, analytics and manufacturing. The field has made significant advances in all of these areas by improving target selection, ADC design, manufacturing methods and clinical strategies. These innovations will inspire and educate scientists who are designing next-generation ADCs with the potential to transform the lives of patients.

Epi-Informatics

Author : Jose Medina-Franco
Publisher : Academic Press
ISBN 13 : 0128028092
Total Pages : 446 pages
Book Rating : 4.1/5 (28 download)

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Book Synopsis Epi-Informatics by : Jose Medina-Franco

Download or read book Epi-Informatics written by Jose Medina-Franco and published by Academic Press. This book was released on 2016-02-24 with total page 446 pages. Available in PDF, EPUB and Kindle. Book excerpt: Epi-Informatics: Discovery and Development of Small Molecule Epigenetic Drugs and Probes features multidisciplinary strategies with strong computational approaches that have led to the successful discovery and/or optimization of compounds that act as modulators of epigenetic targets. This book is intended for all those using or wanting to learn more about computational methodologies in epigenetic drug discovery, including molecular modelers, informaticians, pharmaceutical scientists, and medicinal chemists. With a better understanding of different molecular modeling and cheminformatic approaches, readers can incorporate these techniques into their own drug discovery projects that may involve chemical synthesis and medium- or high-throughput screening. In addition, this book highlights the significance of epigenetic targets to the public health for molecular modelers and chemoinformatians. The goal of this reference is to stimulate ongoing multidisciplinary research and to further improve current computational methodologies and workflows in order to accelerate the discovery and development of epi-drugs and epi-probes. - Focuses on the discovery of epi-drugs as candidates to be used in therapy including combined therapies - Describes new computational methodologies and screening assays utilizing recent and emerging novel structural data - Highlights the discovery, development and optimization of epi-probes, which are molecular probes that elucidate epigenetic mechanisms - Includes important topics such as computational-guided optimization of epi-hits, virtual screening to identify novel compounds for epigenetic targets, development and mining of epigenetic molecular databases, SAR modeling of screening data and much more

Drug Discovery from Mother Nature

Author : Subash Chandra Gupta
Publisher : Springer
ISBN 13 : 3319413422
Total Pages : 411 pages
Book Rating : 4.3/5 (194 download)

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Book Synopsis Drug Discovery from Mother Nature by : Subash Chandra Gupta

Download or read book Drug Discovery from Mother Nature written by Subash Chandra Gupta and published by Springer. This book was released on 2016-10-22 with total page 411 pages. Available in PDF, EPUB and Kindle. Book excerpt: Second comprehensive volume focuses on anti-inflammatory nutraceuticals and their role in prevention and therapy of various chronic diseases. Food and drug administration (FDA) approved drugs such as steroids, non-steroidal anti-inflammatory drugs (NSAIDS), statins and metformin have been shown to modulate inflammatory pathways, but their long-term intake has been associated with numerous side effects. Thus dietary agents which can modulate inflammatory pathways in humans, are likely to exhibit enormous potential. Leading experts describe the latest results of anti-inflammatory nutraceuticals and their role in prevention and therapy of various chronic diseases.

Target Discovery and Validation

Author : Alleyn T. Plowright
Publisher : John Wiley & Sons
ISBN 13 : 3527345299
Total Pages : 396 pages
Book Rating : 4.5/5 (273 download)

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Book Synopsis Target Discovery and Validation by : Alleyn T. Plowright

Download or read book Target Discovery and Validation written by Alleyn T. Plowright and published by John Wiley & Sons. This book was released on 2020-02-18 with total page 396 pages. Available in PDF, EPUB and Kindle. Book excerpt: The modern drug developers? guide for making informed choices among the diverse target identification methods Target Discovery and Validation: Methods and Strategies for Drug Discovery offers a hands-on review of the modern technologies for drug target identification and validation. With contributions from noted industry and academic experts, the book addresses the most recent chemical, biological, and computational methods. Additionally, the book highlights techologies that are applicable to ?difficult? targets and drugs directed at multiple targets, including chemoproteomics, activity-based protein profiling, pathway mapping, genome-wide association studies, and array-based profiling. Throughout, the authors highlight a range of diverse approaches, and target validation studies reveal how these methods can support academic and drug discovery scientists in their target discovery and validation research. This resource: -Offers a guide to identifying and validating targets, a key enabling technology without which no new drug development is possible -Presents the information needed for choosing the appropriate assay method from the ever-growing range of available options -Provides practical examples from recent drug development projects, e. g. in kinase inhibitor profiling Written for medicinal chemists, pharmaceutical professionals, biochemists, biotechnology professionals, and pharmaceutical chemists, Target Discovery and Validation explores the current methods for the identification and validation of drug targets in one comrpehensive volume. It also includes numerous practical examples.

Molecular Recognition of DNA Double Helix

Author : Abhijit Saha
Publisher : Springer
ISBN 13 : 9811087466
Total Pages : 126 pages
Book Rating : 4.8/5 (11 download)

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Book Synopsis Molecular Recognition of DNA Double Helix by : Abhijit Saha

Download or read book Molecular Recognition of DNA Double Helix written by Abhijit Saha and published by Springer. This book was released on 2018-03-22 with total page 126 pages. Available in PDF, EPUB and Kindle. Book excerpt: In this book, the molecular recognition of DNA using small molecules is discussed, with a study of the photochemistry of BrU-labeled DNA. The purposes of the study were to develop small molecules for regenerative medicine, to develop a method to detect the recognition site of small molecules, and to detect the most important biological phenomena using the photochemistry of BrU-labeled DNA. The study began with the design and development of small molecules that can induce pluripotency genes. To deal with the important issue of cell permeability of the original compound, a new analogue of the original with improved gene expression was designed and synthesized. Using the photochemistry of BrU-labeled DNA, crucial biological phenomena such as cooperativity between transcription factors were detected. For the first time, the cooperativity was examined by excess electron transfer assay. DNA was also studied very carefully in order to understand the mechanism of the double-strand break in the UVA micro-irradiation technique. The mechanism of the double strand remained untouched. Nevertheless, the double-strand break mechanism was clearly demonstrated by Hoechst dye, as shown in this book.

Bioactive Natural Products

Author : Goutam Brahmachari
Publisher : World Scientific
ISBN 13 : 9814335371
Total Pages : 695 pages
Book Rating : 4.8/5 (143 download)

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Book Synopsis Bioactive Natural Products by : Goutam Brahmachari

Download or read book Bioactive Natural Products written by Goutam Brahmachari and published by World Scientific. This book was released on 2012 with total page 695 pages. Available in PDF, EPUB and Kindle. Book excerpt: Bioactive natural products are a rich source of novel therapeutics. Thus, the search for bioactive molecules from nature continues to play an important role in fashioning new medicinal agents. This volume, which comprises sixteen chapters written by active researchers and leading experts in natural products chemistry, brings together an overview of current discoveries in this remarkable field. It also provides information on the industrial application of natural products for medicinal purposes. This book will serve as a valuable resource for researchers to predict promising leads for developing pharmaceuticals to treat various ailments and disease manifestations.

How Tobacco Smoke Causes Disease

Author : United States. Public Health Service. Office of the Surgeon General
Publisher :
ISBN 13 :
Total Pages : 728 pages
Book Rating : 4.:/5 (318 download)

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Book Synopsis How Tobacco Smoke Causes Disease by : United States. Public Health Service. Office of the Surgeon General

Download or read book How Tobacco Smoke Causes Disease written by United States. Public Health Service. Office of the Surgeon General and published by . This book was released on 2010 with total page 728 pages. Available in PDF, EPUB and Kindle. Book excerpt: This report considers the biological and behavioral mechanisms that may underlie the pathogenicity of tobacco smoke. Many Surgeon General's reports have considered research findings on mechanisms in assessing the biological plausibility of associations observed in epidemiologic studies. Mechanisms of disease are important because they may provide plausibility, which is one of the guideline criteria for assessing evidence on causation. This report specifically reviews the evidence on the potential mechanisms by which smoking causes diseases and considers whether a mechanism is likely to be operative in the production of human disease by tobacco smoke. This evidence is relevant to understanding how smoking causes disease, to identifying those who may be particularly susceptible, and to assessing the potential risks of tobacco products.

Pharmacoepigenetics

Author : Ramón Cacabelos
Publisher : Academic Press
ISBN 13 : 0128139404
Total Pages : 986 pages
Book Rating : 4.1/5 (281 download)

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Book Synopsis Pharmacoepigenetics by : Ramón Cacabelos

Download or read book Pharmacoepigenetics written by Ramón Cacabelos and published by Academic Press. This book was released on 2019-06-04 with total page 986 pages. Available in PDF, EPUB and Kindle. Book excerpt: Pharmacoepigenetics provides a comprehensive volume on the role of epigenetics and epigenomics in drug discovery and development, providing a detailed, but accessible, view of the field, from basic principles, to applications in disease therapeutics. Leading international researchers from across academia, clinical settings and the pharmaceutical industry discuss the influence of epigenetics and epigenomics in human pathology, epigenetic biomarkers for disease prediction, diagnosis, and treatment, current epigenetic drugs, and the application of epigenetic procedures in drug development. Throughout the book, chapter authors offer a balanced and objective discussion of the future of pharmacoepigenetics and its crucial contribution to the growth of precision and personalized medicine. - Fully examines the influence of epigenetics and epigenomics in human pathology, epigenetic biomarkers for disease prediction, diagnosis, treatment, current epigenetic drugs and the application of epigenetic procedures in drug development - Features chapter contributions from leading international researchers in academia, clinical settings and the pharmaceutical industry - Instructs researchers, students and clinicians on how to better interpret and employ pharmacoepigenetics in drug development, efficiency and safety - Provides a balanced and objective discussion of the future of pharmacoepigenetics and its crucial role in precision medicine