Download or read book Chemical Synthesis of Nucleoside Analogues written by Pedro Merino and published by John Wiley & Sons. This book was released on 2013-02-12 with total page 859 pages. Available in PDF, EPUB and Kindle. Book excerpt: Compiles current tested and proven approaches to synthesize novel nucleoside analogues Featuring contributions from leading synthetic chemists from around the world, this book brings together and describes tested and proven approaches for the chemical synthesis of common families of nucleoside analogues. Readers will learn to create new nucleoside analogues with desired therapeutic properties by using a variety of methods to chemically modify natural nucleosides, including: Changes to the heterocyclic base Modification of substituents at the sugar ring Replacement of the furanose ring by a different carbo- or heterocyclic ring Introduction of conformational restrictions Synthesis of enantiomers Preparation of hydrolitically stable C-nucleosides Chemical Synthesis of Nucleoside Analogues covers all the major classes of nucleosides, including pronucleotides, C-nucleosides, carbanucleosides, and PNA monomers which have shown great promise as starting points for the synthesis of nucleoside analogues. The book also includes experimental procedures for key reactions related to the synthesis of nucleoside analogues, providing a valuable tool for the preparation of a number of different compounds. Throughout the book, chemical schemes and figures help readers better understand the chemical structures of nucleoside analogues and the methods used to synthesize them. Extensive references serve as a gateway to the growing body of original research studies and reviews in the field. Synthetically modified nucleosides have proven their value as therapeutic drugs, in particular as antiviral and antitumor agents. However, many of these nucleoside analogues have undesirable side effects. With Chemical Synthesis of Nucleoside Analogues as their guide, researchers have a new tool for synthesizing a new generation of nucleoside analogues that can be used as therapeutic drugs with fewer unwanted side effects.
Download or read book Reverse Transcriptase Inhibitors in HIV AIDS Therapy written by Gail Skowron and published by Springer Science & Business Media. This book was released on 2007-11-10 with total page 536 pages. Available in PDF, EPUB and Kindle. Book excerpt: A magisterial survey of all aspects of the reverse transcriptase inhibitors (RTIs) used to treat HIV/AIDS, including drug discovery, pharmacology, development of drug resistance, toxicity, and prevention of mother-to-child transmission of HIV/AIDS. The authors synthesize our current understanding of the role of reverse transcriptase in the viral life cycle, describe the discovery and development of eight nucleoside and nucleotide analogs that represent milestones in treatment history, and thoroughly discuss the question of toxicity and resistance to this class of drugs. They also address three non-nucleoside RTIs and their pharmacokinetics and comparative clinical efficacy, new RTIs currently under development, and the impact of approved agents on treatment, in general, and on vertical transmission in the developing world.
Download or read book Nucleoside Analogues written by R. T. Walker and published by Springer Science & Business Media. This book was released on 2012-12-06 with total page 463 pages. Available in PDF, EPUB and Kindle. Book excerpt: This publication contains the Review Lectures given at a joint NATO Advanced Study Institute and a FEB S Advanced Study Course, held at Sogesta (Nr. Urbino), Italy from the 7th - 18th May 1979. The Course entitled "Nucleoside Analogues : Chemistry, Biology and Medical Applications" was held for several reasons. In the past few years, many useful and potentially-useful nucleoside analogues have either reached the stage of clinical use or are undergoing clinical trials. Many more compounds have been synthesised by the organic chemist and little more has been done with them other than possibly a few perfunctory biological tests. This is often due to either a lack of interest or an inadequate knowledge of the testing proced ures available or a lack of communication between the chemist, biochemist, pharmacologist and the clinician such that few compounds receive the testing and evaluation which they deserve. The aim of this meeting was to gather together many of the experts in the different scientific disciplines which are involved in the design, synthesis, testing and clinical use of nucleoside analogues, primarily as anti-viral and anti-cancer agents, and to discuss in depth the fundamental principles of each discipline so that participants could understand each other's problems and be more aware of the information required and that which can be obtained.
Download or read book Enzymatic and Chemical Synthesis of Nucleic Acid Derivatives written by Jesús Fernández Lucas and published by John Wiley & Sons. This book was released on 2019-04-29 with total page 348 pages. Available in PDF, EPUB and Kindle. Book excerpt: A review of innovative tools for creative nucleic acid chemists that open the door to novel probes and therapeutic agents Nucleic acids continue to gain importance as novel diagnostic and therapeutic agents. With contributions from noted scientists and scholars, Enzymatic and Chemical Synthesis of Nucleic Acid Derivatives is a practical reference that includes a wide range of approaches for the synthesis of designer nucleic acids and their derivatives. The book covers enzymatic (including chemo-enzymatic) methods, with a focus on the synthesis and incorporation of modified nucleosides. The authors also offer a review of innovative approaches for the non-enzymatic chemical synthesis of nucleic acids and their analogs and derivatives, highlighting especially challenging species. The book offers a concise review of the methods that prepare novel and heavily modified polynucleotides in sufficient amount and purity for most clinical and research applications. This important book: -Presents a timely and topical guide to the synthesis of designer nucleic acids and their derivatives -Addresses the growing market for nucleotide-derived pharmaceuticals used as anti-infectives and chemotherapeutic agents, as well as fungicides and other agrochemicals. -Covers novel methods and the most recent trends in the field -Contains contributions from an international panel of noted scientistics Written for biochemists, medicinal chemists, natural products chemists, organic chemists, and biotechnologists, Enzymatic and Chemical Synthesis of Nucleic Acid Derivatives is a practice-oriented guide that reviews innovative methods for the enzymatic as well as non-enzymatic synthesis of nucleic acid species.
Download or read book Nucleoside Triphosphates and their Analogs written by Morteza Vaghefi and published by CRC Press. This book was released on 2016-04-19 with total page 408 pages. Available in PDF, EPUB and Kindle. Book excerpt: While adenosine triphosphate (ATP) is described as the universal currency of energy in all living organisms at the cellular level, the actual power lies in its phosphate tail. This book is the first dedicated to the field of nucleoside triphosphate (NTP). Its 13 chapters encompass the contributions of twenty scientists from both academia and industry. It provides collective information on the chemical, physiochemical, and biological properties of both natural and modified NTP and their application in life sciences. Three chapters review families of enzymes that depend on nucleotides for assembling DNA and RNA molecules. The appendix includes supporting NMR data.
Download or read book Palladium Catalyzed Modification of Nucleosides Nucleotides and Oligonucleotides written by Anant R. Kapdi and published by Elsevier. This book was released on 2018-06-04 with total page 360 pages. Available in PDF, EPUB and Kindle. Book excerpt: Palladium-Catalyzed Modification of Nucleosides, Nucleotides and Oligonucleotides describes the procedures and protocols related to the modification of nucleosides, nucleotides and oligonucleotides via Pd-mediated cross-coupling processes. The book highlights the growing area of nucleic acid modification and how Pd-mediated coupling reactions can assist this development. Users will find key synthetic protocols for these reactions in this latest volume in the Latest Trends in Palladium Chemistry series. As most of the research in the field of antiviral agents has centered on the use of modified nucleosides that have exhibited promising activity, this book provides an up-to-date reference for both professionals in industry and other interested parties. - Provides synthetic routes for useful nucleoside molecules, information otherwise found only through time-consuming literature searches - Covers metal-mediated and metal-catalyzed cross coupling processes of nucleosides and related compounds - Includes Suzuki-Miyaura, Stille and Sonogashira reactions, as well as C-H bond functionalization - Highlights the growing area of nucleic acid modification and how Pd-mediated coupling reactions can assist
Download or read book Review of the Fialuridine FIAU Clinical Trials written by Institute of Medicine and published by National Academies Press. This book was released on 1995-03-14 with total page 279 pages. Available in PDF, EPUB and Kindle. Book excerpt: In June 1993 a clinical trial of fialuridine (FIAU), a promising new medication for hepatitis B, was abruptly terminated when one of the 15 out-patients participating in the National Institutes of Health (NIH) study was suddenly hospitalized with liver failure. Although all the remaining patients were contacted and told to stop taking their medication, six more subsequently developed severe toxicity. Five patients died, and two others were probably saved from death only by having liver transplants. In response to a request from the Secretary of the Department of Health and Human Services, the IOM committee has analyzed the FIAU clinical trials, making recommendations for additional safeguards for the conduct of future clinical trials. This evaluation included the review of documents pertaining to investigational new drug submissions, protocols and consent forms from other clinical trials, as well as information available from other clinical and preclinical experience with compounds related to FIAU and its parent drug, fiacitibine (FIAC), which is metabolized to FIAU. The committee does not seek to affix responsibility for the adverse outcome of this NIH trial, but instead focuses on whether any rules or procedures governing the clinical trials process itself need to be changed, and if so, what burdens or costs such changes might place on future clinical trials.
Download or read book Chronic Lymphoid Leukemias Second Edition written by Bruce D. Cheson and published by CRC Press. This book was released on 2001-04-25 with total page 664 pages. Available in PDF, EPUB and Kindle. Book excerpt: Written by over 50 internationally distinguished experts, 30 more than the first edition, and contains nine new chapters! Continuing in the esteemed tradition and heralded success of the first edition, Chronic Lymphoid Leukemias, Second Edition offers a full overview of chronic lymphocytic leukemia (CLL) from multiple perspectives-covering all major developments since the previous edition was published eight years ago. Chronicling the complete history and variations of CLL-type leukemia, the Second Edition reviews the origin, nature, and molecular differences between B-CLL and T-CLL/PLL leukemias analyzes core constituents of apoptosis and causes for dysregulation of programmed cell death (PCD) in B-CLL examines recent research on the role cytokines and regulatory molecules may play in cross-cell communication profiles commonly used vectors for somatic gene therapy, as well as the latest advances in genetic engineering and vector design and production utilizes up-to-the-minute techniques such as fluorescence in-situ hybridization (FISH) and comparative genomic hybridization (CGH) to detect genetic abnormalities and aberrations explores current measures of supportive care with splenectomy, cytokine proteins, and intravenous immunoglobulin applications identifies how to manage infectious and psychiatric complications in patients with CLL and much more! Provides contemporary results on the efficacy of nucleoside analog combinations such as ara-C with fludarabine and cladribine and on the emerging nucleosides nelarabine and clofarabine! Copiously supplemented with over 2500 literature references-1000 more than the first edition-Chronic Lymphoid Leukemias, Second Edition fulfills the reference needs of oncologists, hematologists, immunologists, pathologists, infectious disease specialists, internists, molecular biologists, and medical school students in these disciplines.
Download or read book Chemistry and Application of H Phosphonates written by Kolio D. Troev and published by Elsevier. This book was released on 2006-09-25 with total page 308 pages. Available in PDF, EPUB and Kindle. Book excerpt: Chemistry and Application of H-Phosphonates is an excellent source for those planning the synthesis of new phosphorus-containing compounds and in particular derivatives containing a phosphonate, phosphoramide or phosphonic acid diester group. The rich chemistry, low cost and easy availability of diesters of H-phosphonic acid makes them an excellent choice as synthone in a number of practically important reactions. Phosphonic acid esters are intermediates in the synthesis of important classes of compounds such as alpha-aminophosphonic acids, bisphosphonates, epoxyalkylphosphonates, alpha-hydroxyalkylphosphonates, phosphoramides, poly(alkylene H-phosphonate)s, poly(alkylene phosphate)s, nucleoside H-phosphonates. The synthesis of each of these compound classes is reviewed in detail. Alpha-Aminophosphonic acids are an important class of biologically active compounds, which have received an increasing amount of attention because they are considered to be structural analogues of the corresponding Alpha-amino acids. The utilities of alpha-aminophosphonates as peptide mimics, haptens of catalytic antibodies, enzyme inhibitors, inhibitors of cancers, tumours, viruses, antibiotics and pharmacologic agents are well documented. Alpha-Hydroxyalkanephosphonates are compounds of significant biological and medicinal applications. Dialkyl epoxyalkylphosphonates are of interest because of their use as intermediates in the synthesis of bioactive substances, and as modifiers of natural and synthetic polymers. Bisphosphonates are drugs that have been widely used in different bone diseases, and have recently been used successfully against many parasites. Poly(alkylene H-phosphonate)s and poly(alkylene phosphate)s are promising, biodegradable, water soluble, new polymer-carriers of drugs. Nucleoside H-phosphonates seem to be the most attractive candidates as starting materials in the chemical synthesis of DNA and RNA fragments. The 5'-hydrogen phosphonate-3'-azido-2',3'-dideoxythimidine is one of the most significant anti-HIV prodrug, which is currently in clinical trials. Chapters review the synthesis; physical and spectral properties (1H, 13C, 31P and 17O NMR data); characteristic reactions; important classes of compounds based on these esters of H-phosphonic acid; their application as physiologically active substances, flame retardants, catalysts, heat and light stabilizers, lubricants, scale inhibitors, polymer-carriers of drugs; preparation of H-phosphonate diesters and general procedures for conducting the most important reactions.* provides ideas for the synthesis of phosphonates, phosphoramides and diesters of phosphonic acid (new phosphorus-containing compounds)* reviews structure, spectra and biological activity of H-phosphonates and their derivatives* examines new areas of application of phosphorus-containing compounds
Download or read book Quasispecies From Theory to Experimental Systems written by Esteban Domingo and published by Springer. This book was released on 2016-03-18 with total page 360 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume brings together recent developments in quasispecies theory extended to variable environments and practical applications in elucidating viral dynamics and treatment designs. In particular, the existence of an error threshold in rugged fitness landscapes has opened the way to a new antiviral strategy termed lethal mutagenesis, which is now under intensive theoretical, experimental and clinical investigation. As such the book explains how an understanding of quasispecies dynamics within infected organisms has increased our knowledge of viral disease events. From a clinical perspective, population dynamics highlights important problems for viral disease control, such as the selection of drug-resistant mutants that often accompanies treatment failures, and suggests means of increasing the effectiveness of antiviral treatments. The book is intended for students and scientists interested in basic and applied aspects of biophysics, chemistry, biology, evolution and medical virology.
Download or read book Mitochondrial Dysfunction Caused by Drugs and Environmental Toxicants written by Yvonne Will and published by John Wiley & Sons. This book was released on 2018-03-23 with total page 816 pages. Available in PDF, EPUB and Kindle. Book excerpt: Developed as a one-stop reference source for drug safety and toxicology professionals, this book explains why mitochondrial failure is a crucial step in drug toxicity and how it can be avoided. • Covers both basic science and applied technology / methods • Allows readers to understand the basis of mitochondrial function, the preclinical assessments used, and what they reveal about drug effects • Contains both in vitro and in vivo methods for analysis, including practical screening approaches for drug discovery and development • Adds coverage about mitochondrial toxicity underlying organ injury, clinical reports on drug classes, and discussion of environmental toxicants affecting mitochondria
Download or read book Antiviral Nucleosides written by C.K. Chu and published by Elsevier. This book was released on 2003-10-15 with total page 269 pages. Available in PDF, EPUB and Kindle. Book excerpt: • Up-to-date review on the chemistry and biology of nucleosides • Modern synthetic methodology • Comprehensive coverage of antiviral nucleosidesThis book summarizes the recent advances in nucleosides chemistry and chemotherapy over the past 10-15 years. It covers recently discovered nucleoside antiviral agents, their therapeutic aspects and biochemistry, and also extensive reviews on their chiral synthesis.
Download or read book Synthesis of Therapeutic Oligonucleotides written by Satoshi Obika and published by Springer. This book was released on 2018-12-08 with total page 280 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book presents the latest knowledge on a broad range of topics relating to the synthesis of natural and artificial oligonucleotides with therapeutic potential. Nucleic acid-based therapeutics are attracting much attention, and numerous therapeutic oligonucleotides, such as antisense oligonucleotides, siRNAs, splice-switching oligonucleotides, and nucleic acid aptamers, are being evaluated in clinical trials for the treatment of a variety of diseases. Synthesis of Therapeutic Oligonucleotides covers a broad range of topics in the field that are of high relevance to researchers, including the synthesis of natural and chemically modified oligonucleotides, the development of novel nucleic acid analogs, industrial scale synthesis and purification of oligonucleotides, and important aspects of chemistry, manufacturing, and controls (CMC). The aim is to provide new insights and inspire fresh ideas in nucleic acid chemistry that may ultimately lead to novel concepts and techniques and the discovery of more effective nucleic acid drugs. The book will be of high value for both established researchers in the field and students intending to specialize in nucleic acid chemistry research.
Download or read book DNA Repair in Cancer Therapy written by Mark R. Kelley and published by Academic Press. This book was released on 2016-06-07 with total page 466 pages. Available in PDF, EPUB and Kindle. Book excerpt: DNA Repair and Cancer Therapy: Molecular Targets and Clinical Applications, Second Edition provides a comprehensive and timely reference that focuses on the translational and clinical use of DNA repair as a target area for the development of diagnostic biomarkers and the enhancement of cancer treatment. Experts on DNA repair proteins from all areas of cancer biology research take readers from bench research to new therapeutic approaches. This book provides a detailed discussion of combination therapies, in other words, how the inhibition of repair pathways can be coupled with chemotherapy, radiation, or DNA damaging drugs. Newer areas in this edition include the role of DNA repair in chemotherapy induced peripheral neuropathy, radiation DNA damage, Fanconi anemia cross-link repair, translesion DNA polymerases, BRCA1-BRCA2 pathway for HR and synthetic lethality, and mechanisms of resistance to clinical PARP inhibitors. - Provides a comprehensive overview of the basic and translational research in DNA repair as a cancer therapeutic target - Includes timely updates from the earlier edition, including Fanconi Anemia cross-link repair, translesion DNA polymerases, chemotherapy induced peripheral neuropathy, and many other new areas within DNA repair and cancer therapy - Saves academic, medical, and pharma researchers time by allowing them to quickly access the very latest details on DNA repair and cancer therapy - Assists researchers and research clinicians in understanding the importance of the breakthroughs that are contributing to advances in disease-specific research
Download or read book Nucleoside Analogs in Cancer Therapy written by Bruce D. Cheson and published by CRC Press. This book was released on 2021-10-28 with total page 494 pages. Available in PDF, EPUB and Kindle. Book excerpt: Offering the most current and complete coverage of nucleoside analog activity in oncology and hematology, this single-source volume includes topics from pharmacology to previously unpublished clinical findings on the pivotal role of fludarabine, cladribine, and pentostatin in the management of diseases, such as chronic lymphocytic and hairy cell leukemia, non-Hodgkin's lymphoma, membranous nephropathy, and rheumatoid and psoriatic arthritis.
Download or read book Targeted Biomarker Quantitation by LC MS written by Naidong Weng and published by John Wiley & Sons. This book was released on 2017-07-31 with total page 397 pages. Available in PDF, EPUB and Kindle. Book excerpt: The first book to offer a blueprint for overcoming the challenges to successfully quantifying biomarkers in living organisms The demand among scientists and clinicians for targeted quantitation experiments has experienced explosive growth in recent years. While there are a few books dedicated to bioanalysis and biomarkers in general, until now there were none devoted exclusively to addressing critical issues surrounding this area of intense research. Target Biomarker Quantitation by LC-MS provides a detailed blueprint for quantifying biomarkers in biological systems. It uses numerous real-world cases to exemplify key concepts, all of which were carefully selected and presented so as to allow the concepts they embody to be easily expanded to future applications, including new biomarker development. Target Biomarker Quantitation by LC-MS primarily focuses on the assay establishment for biomarker quantitation—a critical issue rarely treated in depth. It offers comprehensive coverage of three core areas of biomarker assay establishment: the relationship between the measured biomarkers and their intended usage; contemporary regulatory requirements for biomarker assays (a thorough understanding of which is essential to producing a successful and defendable submission); and the technical challenges of analyzing biomarkers produced inside a living organism or cell. Covers the theory of and applications for state-of-the-art mass spectrometry and chromatography and their applications in biomarker analysis Features real-life examples illustrating the challenges involved in target biomarker quantitation and the innovative approaches which have been used to overcome those challenges Addresses potential obstacles to obtain effective biomarker level and data interpretation, such as specificity establishment and sample collection Outlines a tiered approach and fit-for-purpose assay protocol for target biomarker quantitation Highlights the current state of the biomarker regulatory environment and protocol standards Target Biomarker Quantitation by LC-MS is a valuable resource for bioanalytical scientists, drug metabolism and pharmacokinetics scientists, clinical scientists, analytical chemists, and others for whom biomarker quantitation is an important tool of the trade. It also functions as an excellent text for graduate courses in pharmaceutical, biochemistry and chemistry.
Download or read book Some Antiviral and Antineoplastic Drugs and Other Pharmaceutical Agents written by IARC Working Group on the Evaluation of Carcinogenic Risks to Humans and published by World Health Organization. This book was released on 2000 with total page 536 pages. Available in PDF, EPUB and Kindle. Book excerpt: Evaluates the carcinogenic risks to humans posed by the use of four antiretroviral agents four DNA topoisomerase II inhibitors used in the treatment of cancer and an additional three pharmaceutical agents (hydroxyures phenolphthalein and vitamin K substances). The volume marks the first IARC evaluation of nucleoside analogs that act as antiviral agents. The evaluation responds in part to recent findings that zidovudine (AZT) an effective antiretroviral agent now being given to pregnant HIV-infected women to prevent maternal-to-fetal transmission of the virus is a transplacental carcinogen in mice. The opening monograph evaluates the carcinogenicity to humans of the antiretroviral nucleoside analogs zidovudine (AZT) zalcitabine (ddC) and didanosine (ddI) and the antiherpesvirus drug aciclovir. Of these aciclovir and didanosine could not be classified on the basis of available data. For zidovudine transplacental administration to mice resulted in an increased incidence and multiplicity of lung and liver tumours and in an increased incidence of female reproductive tract tumours in one study but not in another involving treatment at a lower dose. Despite observation of toxic effects in some studies of humans human carcinogenicity data were judged to provide inadequate evidence of carcinogenicity in humans. Zidovudine was classified as possibly carcinogenic to humans. Similar weaknesses in human carcinogenicity data for zalcitabine which consistently induces thymic lymphomas in mice resulted in its classification as possibly carcinogenic to humans. The second monograph evaluates four DNA topoisomerase II inhibitors: etoposide teniposide mitoxantrone and amsacrine. Of these etoposide - one of the most widely used and effective cytotoxic drugs in combination therapy - was classified as probably carcinogenic to humans and etoposide in combination with cisplatin and bleomycin was judged to be carcinogenic to humans. Teniposide was classified as probably carcinogenic to humans and mitoxantrone and amsacrine were classified as possibly carcinogenic to humans. Of the three pharmaceutical agents evaluated in the final monograph hydroxyurea which is widely used in cancer treatment and increasingly in combination with didanosine in HIV infection could not be classified. Phenolphthalein a widely used laxative now being withdrawn from the market in many countries because of toxicological concerns was classified as possibly carcinogenic. Vitamin K substances could not be classified on the basis of available evidence.
