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Author: Claire Simons
Publisher: CRC Press
ISBN: 9789056993245
Category : Medical
Languages : en
Pages : 206
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Book Description
Nucleosides exhibit a broad spectrum of biological activity that generally results from their ability to inhibit specific enzymes. This activity has led to their use in the development of various pharmaceutical agents used in the treatment of cancers and to combat harmful viruses, bacteria and parasites. Nucleoside Mimetics provides an introduction to the chemistry of nucleoside mimetics, which combines carbohydrate, heterocyclic and asymmetric synthesis. The book gives a comprehensive introduction to nucleosides and coverage of the various classes. The aim of Nucleoside Mimetics is to provide the reader with a useful insight into the diversity of nucleosides, the range of elegant chemistry involved and the continuing importance of nucleosides as both therapeutic agents and as probes for studying biochemical processes.
Author: Claire Simons
Publisher: CRC Press
ISBN: 9789056993245
Category : Medical
Languages : en
Pages : 206
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Book Description
Nucleosides exhibit a broad spectrum of biological activity that generally results from their ability to inhibit specific enzymes. This activity has led to their use in the development of various pharmaceutical agents used in the treatment of cancers and to combat harmful viruses, bacteria and parasites. Nucleoside Mimetics provides an introduction to the chemistry of nucleoside mimetics, which combines carbohydrate, heterocyclic and asymmetric synthesis. The book gives a comprehensive introduction to nucleosides and coverage of the various classes. The aim of Nucleoside Mimetics is to provide the reader with a useful insight into the diversity of nucleosides, the range of elegant chemistry involved and the continuing importance of nucleosides as both therapeutic agents and as probes for studying biochemical processes.
Author: Andrew Stephen Rowan
Publisher:
ISBN:
Category :
Languages : en
Pages :
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Book Description
Author: Pedro Merino
Publisher: John Wiley & Sons
ISBN: 1118498100
Category : Science
Languages : en
Pages : 859
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Book Description
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.
Author: Jesús Fernández Lucas
Publisher: John Wiley & Sons
ISBN: 3527343768
Category : Science
Languages : en
Pages : 348
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Book Description
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.
Author: Marco Brito-Arias
Publisher: Springer Nature
ISBN: 3030978540
Category : Science
Languages : en
Pages : 543
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Book Description
This third edition is a comprehensive and extended study about the best known approaches for preparing the main types of glycosides, covering the classic and more recent glycosylation reactions used for preparing simple and challenging glycosides currently used as potent antiviral and antineoplastic drugs, or fluorogenic substrates used for enzymatic detection in cell biology. Besides, this new edition provides more examples of the glycosidic methodologies followed for preparing complex glycoconjugates such as glycoproteins and glycosphingolipids and gangliosides used as adjuvants or as synthetic vaccines candidates. Also, additional mechanistic evidence is presented for better understanding of the glycosylation reaction, trying to identify the variables mainly depending on protecting and leaving groups, as well as catalyst and reaction condition which altogether directs the anomeric stereo control. A chapter on the glycoside hydrolysis is included in view of the increasing interest in the use of biomass as a natural and renewable source for obtaining important intermediates or products used in food or valuable materials. The author includes information in the characterization of glycosides section with the aim of giving additional tools for the structural assignment through NMR, X-Ray and mass spectra techniques.
Author: Godefridus J Peters
Publisher: Springer Science & Business Media
ISBN: 1597451487
Category : Medical
Languages : en
Pages : 482
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Book Description
Successful cancer chemotherapy relies heavily on the application of various deoxynucleoside analogs. Since the very beginning of modern cancer chemotherapy, a number of antimetabolites have been introduced into the clinic and subsequently applied widely for the treatment of many malignancies, both solid tumors and hematological disorders. In the latter diseases, cytarabine has been the mainstay of treatment of acute myeloid leukemia. Although many novel compounds were synthesized in the 1980s and 1990s, no real improvement was made. However, novel technology is now capable of elucidating the molecular basis of several inborn errors as well as some specific malignancies. This has enabled the synthesis of several deoxynucleoside analogs that could be applied for specific malignancies, such as pentostatin and subsequently chlorodeoxyadenosine (cladribine) for the treatment of hairy cell leukemia. Already in the early stage of deoxynucleoside analog development, it was recognized that several of these compounds were very effective in the treatment of various viral infections, such as for the treatment of herpes infections. This formed the basis initially for the design of azidothymidine and subsequently many other analogs, which are currently successfully used for the treatment of HIV infections. As a spin-off of these research lines, some compounds not eligible for development as antiviral agents appeared to be very potent anticancer agents. The classical example is gemcitabine, now one of the most widely applied deoxynucleoside analogs, used for the (combination) treatment of non-small cell lung cancer, pancreatic cancer, bladder cancer, and ovarian cancer.
Author: H. Jphn Smith
Publisher: CRC Press
ISBN: 0203304152
Category : Medical
Languages : en
Pages : 684
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Book Description
Advances in knowledge and technology have revolutionized the process of drug development, making it possible to design drugs for a given target or disease. Building on the foundation laid by the previous three editions, Smith and Williams Introduction to the Principles of Drug Design and Action, Fourth Edition includes the latest informatio
Author: Piet Herdewijn
Publisher: Springer Science & Business Media
ISBN: 1592598234
Category : Medical
Languages : en
Pages : 436
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Book Description
A collection of powerful new techniques for oligonucleotide synthesis and for the use of modified oligonucleotides in biotechnology. Among the protocol highlights are a novel two-step process that yields a high purity, less costly, DNA, the synthesis of phosphorothioates using new sulfur transfer agents, the synthesis of LNA, peptide conjugation methods to improve cellular delivery and cell-specific targeting, and triple helix formation. The applications include using molecular beacons to monitor the PCR amplification process, nuclease footprinting to study the sequence-selective binding of small molecules of DNA, nucleic acid libraries, and the use of small interference RNA (siRNA) as an inhibitor of gene expression.
Author: E. De Clercq
Publisher: Elsevier
ISBN: 0080522262
Category : Science
Languages : en
Pages : 231
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Book Description
The fourth volume of Advances in Antiviral Drug Design is keeping up with the recent progress made in the broad field of antiviral drug research and encompasses six specific directions that have opened new avenues for the treatment of HIV and other virus infections.First, as the introductory chapter, the different new anti-HIV agents that are now in preclinical or clinical development are reviewed by E. De Clercq. This includes new NRTIs, NNRTIs and PIs, but also HIV entry/fusion inhibitors as well as integrase inhibitors, and some of these agents, such as the NRTI emtricitabine [(-)FTC] and the PI atazanavir, may soon be licensed for clinical use.Second, high expectations are vested in the potential therapeutic usefulness of inhibitors of HIV integration, a point of no return in the life cycle of HIV, and this approach is highlighted by D.J. Hazuda and S.D. Young.Third, as all currently available PIs can be described as "peptidomimetic", and, therefore, expected to demonstrate overlapping virus-drug resistance and side effect profiles, it would be interesting to see how a non-peptidic protease inhibitor such as tipranavir behaves, and this is covered by D. Mayers, K. Curry, V. Kohlbrenner and S. McCallister.Fourth, neuraminidase inhibitors such as zanamivir (that has to be inhaled) and oseltamivir (that can be administered via the oral route) have gained a definitive status as antiviral drugs useful for both therapy and prophylaxis of influenza A and B virus infections; as they target a specific influenza viral enzyme, neuraminidase (or sialidase), they may be expected to block newly emerging influenza viruses as well, and the design of neuraminidase inhibitors has received due attention of H. Jin and C.U. Kim.Fifth, while the major current efforts in antiviral drug development have shifted from herpesviruses towards HIV and hepatitis viruses [hepatitis B virus (HBV), hepatitis C virus (HCV)], it is interesting to note that by switching from the classical five-membered sugar or acyclic nucleoside strategy, J. Wang, M. Froeyen and P. Herdewijn have gone "upstream" in designing six-membered carbocyclic nucleosides as potential anti-herpesvirus agents.Sixth, following up on the nucleotide prodrug strategy introduced above under ix, to deliver the biologically active nucleotides inside the cells, C. Meier has elaborated on a particular class of such pronucleotides, namely that of the cyclosaligenyl pronucleotides, an approach that should have far reaching implications for compounds effective against HIV, HBV and other viruses.The six topics covered in this fourth volume of Advances in Antiviral Drug Design are in the front line of the present endeavors towards the design and development of new therapeutic agents for virus infections. They pertain to the combat against three of the most important viral pathogens of current times: HIV, HBV, influenza virus and herpesviruses.
Author: Galal H. Elgemeie
Publisher: Elsevier
ISBN: 0128217847
Category : Science
Languages : en
Pages : 630
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Book Description
New Strategies Targeting Cancer Metabolism: Anticancer Drugs, Synthetic Analogues and Antitumor Agents presents up-to-date synthetic strategies for three categories of antimetabolites: antifolates, purines and pyrimidines, the main classes of antimetabolites which are integrated into various pharmaceutical agents. Many of these antimetabolites are considered potent chemotherapeutic agents which have great potential impact on medical research. These main classes of antimetabolites are used in the treatment of critical diseases including cancer, malignancies, autoimmune diseases, and many other non-malignant diseases. Antineoplastic drugs such as alkylating agents which have significant effects are described. Novel synthetic strategies for many anticancer alkylating agents including nitrogen mustards, chlorambucil, melphalan, ifosamide, oxaliplatin and temozolomide are explored. Natural products have offered some of the most significant drugs for treating cancer, as many drugs currently in clinical use are derived from natural products as camptothecins, vinca alkaloids, and derivatives of podophyllotoxin. They provide a contribution that is essential for modern drug discovery and development. In this book, insights into a broad array of novel compounds are reviewed, well-recognized synthetic approaches are emphasized for further anticancer drug development and discovery, and the biological evaluation of novel synthesized compounds are included. This comprehensive reference is a valuable resource for medical chemists working in drug discovery and development, as well as pharmacologists and biochemists working in related fields. - Provides the only resource dedicated to synthetic strategies of antimetabolites - Features synthetic strategies for nucleosides and their analogues - Includes coverage of purine-, pyrimidine- and antifolate-based anticancer drugs - The most significant anticancer alkylating agents and natural products are demonstrated
