Nucleoside Analogues
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Nucleoside Analogues
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Author : R. T. Walker
language : en
Publisher: Springer Science & Business Media
Release Date : 2012-12-06
Nucleoside Analogues written by R. T. Walker and has been published by Springer Science & Business Media this book supported file pdf, txt, epub, kindle and other format this book has been release on 2012-12-06 with Science categories.
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.
Chemical Synthesis Of Nucleoside Analogues
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Author : Pedro Merino
language : en
Publisher: John Wiley & Sons
Release Date : 2013-02-12
Chemical Synthesis Of Nucleoside Analogues written by Pedro Merino and has been published by John Wiley & Sons this book supported file pdf, txt, epub, kindle and other format this book has been release on 2013-02-12 with Science categories.
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.
Nucleoside Analogues
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Author : Erik de Clercq
language : en
Publisher:
Release Date : 1979
Nucleoside Analogues written by Erik de Clercq and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 1979 with categories.
Nucleotide Analogues As Antiviral Agents
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Author : John C. Martin
language : en
Publisher:
Release Date : 1989
Nucleotide Analogues As Antiviral Agents written by John C. Martin and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 1989 with Language Arts & Disciplines categories.
Largely in response to the AIDS epidemic, the amount of research directed toward the discovery of antiviral agents has greatly expanded. This new volume focuses on the potential of nucleotides to exert potent in vivo antiviral effects. It presents the findings of an international group of scientists who are carrying out research at the forefront of the nucleotide drug design. Twelve chapters describe many new concepts and results, much of which has been previously unpublished. This book assembles a valuable collection of information, offering insight into this increasingly important research topic.
Nucleoside Analogues
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Author : Richard T. Walker
language : en
Publisher:
Release Date : 1979
Nucleoside Analogues written by Richard T. Walker and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 1979 with categories.
Nucleoside Triphosphates And Their Analogs
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Author : Morteza Vaghefi
language : en
Publisher: CRC Press
Release Date : 2016-04-19
Nucleoside Triphosphates And Their Analogs written by Morteza Vaghefi and has been published by CRC Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 2016-04-19 with Medical categories.
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.
Nucleoside Analogs In Cancer Therapy
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Author : Bruce D. Cheson
language : en
Publisher: CRC Press
Release Date : 2021-10-28
Nucleoside Analogs In Cancer Therapy written by Bruce D. Cheson and has been published by CRC Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 2021-10-28 with Medical categories.
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.
Diastereoselective Synthesis Of Nucleoside Analogues Via Cyclization Of Acyclic Precursors
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Author : Starr Dostie
language : en
Publisher:
Release Date : 2016
Diastereoselective Synthesis Of Nucleoside Analogues Via Cyclization Of Acyclic Precursors written by Starr Dostie and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 2016 with categories.
"Effective treatments against cancer and viral infections involve the administration of modified nucleosides that act as inhibitors of tumor growth and viral replication. The existing paradigm that governs nucleoside synthesis requires addition of nucleobases onto activated cyclic glycosyl donors. In such cases, the stereoselectivities depend on steric effects, anchimeric participation or displacement of an anomeric halide. A novel approach to nucleoside analogue synthesis using chiral acyclic thioaminals has been developed by our laboratory. A kinetically controlled cyclization of an acyclic precursor already containing the nucleobase is well suited to create such sterically encumbered molecules. Such cyclizations involve a stereogenic center bearing the nucleobase and a thioether moiety. This thioether may serve as a leaving group or as a nucleophile. In order to take advantage of the stereochemistry of the thioaminal at C1, both types of cyclizations involve intramolecular SN2-like nucleophilic displacements. The first cyclization involves displacement of the activated thioalkyl group of the thioaminal by the secondary hydroxyl group at C4 (O4′-C1 cyclization) resulting in D-1',2'-trans furanosides. Alternatively, the sulfur of the thioaminal can serve as a nucleophile when the C4 hydroxyl is converted into a leaving group (S1′-C4 cyclization). This strategy gives access to L-1',2'-cis thioanalogues. This acyclic approach addresses two key synthetic challenges in the synthesis of nucleoside analogues, namely, formation of L-nucleoside analogues along with a 1',2'-cis stereochemical arrangement between the nucleobase and the C2'-substituent. A protocol was developed in which acyclic N,OTMS-acetals were accessed with high 1,2-syn diastereoselectivities by addition of silylated pyrimidine and adenine nucleobases onto aldehydes in the presence of a bidentate Lewis acid. In the subsequent O1'-C4 cyclization, the oxygen of the acetal serves as the nucleophile involved in the displacement of the leaving group at the C4 position. This strategy provides stereoselective access to unnatural L-nucleosides with a variety of nucleobases starting from easily accessible pools of D-sugars. As importantly, this methodology addresses the challenging synthesis of 1',2'-cis nucleosides. The efficient synthesis of nucleoside analogues using this acyclic methodology relies on introduction of a pyrimidine or purine nucleobase in a stereocontrolled manner onto an acyclic precursor. It has been observed that nucleobases add to C2-alkoxydithioacetals with high 1,2-syn selectivity. An experimental and theoretical model compound study has been done to rationalize the origin of this 1,2-syn diastereocontrol (anti-Felkin-Anh) when silylated nucleobases add to acyclic dithioacetals. A modification that improves the biological properties of nucleoside analogues is the introduction of fluorine, a common tool used in drug discovery. Access to two of the scaffolds that are difficult to synthesize using standard paradigms for nucleoside analogue formation, namely, 1',2'-trans furanosides and 1',2'-cis thiofuranosides bearing a fluorine in the C2'-position is possible using our acyclic approach. Nucleobase coupling onto acyclic dithioacetals bearing a C2-F maintains preference for 1,2-syn stereocontrol and subsequent intramolecular cyclization of these fluorinated thioaminals provides 1',2'-trans furanosides and 1',2'-cis-thiofurnaosides. Using these C2'-F scaffolds formation of SAM analogues, the cofactor implicated in methyltransferases, were designed.Despite the availability of nucleoside analogues, there is a need to develop new agents with improved properties to overcome issues of resistance. In this regard, a new series of NAs bearing a C3'-quaternary center and a C2'-F atom have been synthesized and are being investigated as potential antimetabolites." --
Reverse Transcriptase Inhibitors In Hiv Aids Therapy
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Author : Gail Skowron
language : en
Publisher: Springer Science & Business Media
Release Date : 2007-11-10
Reverse Transcriptase Inhibitors In Hiv Aids Therapy written by Gail Skowron and has been published by Springer Science & Business Media this book supported file pdf, txt, epub, kindle and other format this book has been release on 2007-11-10 with Medical categories.
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.
I Triazine Nucleoside Analogues
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Author : Michelle Hysell
language : en
Publisher:
Release Date : 2004
I Triazine Nucleoside Analogues written by Michelle Hysell and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 2004 with categories.