Medicinal chemistry of bioactive natural products [[electronic resource] /] / edited by Xiao-Tian Liang, Wei-Shuo Fang

• Record Nr.: UNINA9910830389103321
• Pubbl/distr/stampa: Hoboken, N.J., : Wiley-Interscience/John Wiley, c2006
• ISBN: 1-280-40909-6; 9786610409099; 0-470-36036-4; 0-471-73934-0; 0-471-73933-2
• Descrizione fisica: 1 online resource (482 p.)
• Altri autori (Persone): LiangXiaotian; FangWei-Shuo
• Disciplina: 615.321; 615/.321
• Soggetti: Materia medica, Vegetable; Pharmaceutical chemistry; Natural products; Bioactive compounds
• Lingua di pubblicazione: Inglese
• Formato: Materiale a stampa
• Livello bibliografico: Monografia
• Note generali: Description based upon print version of record.
• Nota di bibliografia: Includes bibliographical references and index.
• Nota di contenuto: MEDICINAL CHEMISTRY OF BIOACTIVE NATURAL PRODUCTS; CONTENTS; Preface; Contributors; 1 The Chemistry and Biology of Epothilones-Lead Structures for the Discovery of Improved Microtubule Inhibitors; 1.1. Introduction; 1.2. Biological Effects of Epo B; 1.2.1 In Vitro Activity; 1.2.2 In Vivo Antitumor Activity; 1.3. Epothilone Analogs and SAR Studies; 1.3.1 Lactam-Based Analogs; 1.3.2 Modifications in the C9-C11 Region; 1.3.3 Modifications of the Epoxide Moiety; 1.3.4 C-26-Modified Analogs; 1.3.5 Side-Chain Modifications; 1.3.6 Aza-Epothilones; 1.4. Pharmacophore Modeling and Conformational Studies1.5. Epothilone Analogs in Clinical Development; 1.6. Conclusions; Acknowledgments; References; 2 The Chemistry and Biology of Vancomycin and Other Glycopeptide Antibiotic Derivatives; 2.1. Introduction; 2.2. Classification of Glycopeptide Antibiotics; 2.3. Mode ; of Action; 2.4. Glycopeptide Resistance; 2.5. Biosynthesis; 2.6. Total Synthesis; 2.7. Glycopeptides as Chiral Selectors in Chromatography and Capillary Electrophoresis; 2.8. Structural Modifications of Glycopeptide Antibiotics and Structure Activity Relationship (SAR) Studies; 2.8.1 Modifications of Glycopeptide Antibiotics2.8.2 Rational Concepts for the Design of Novel Glycopeptides; 2.8.3 Conclusions; Acknowledgment; References; 3 Structure Modifications and Their Influences on Antitumor and Other Related Activities of Taxol and Its Analogs; 3.1. Discovery and Research and Development of Taxol; 3.2. Paclitaxel Analogs Active Against Normal Tumor Cells; 3.2.1 C-13 Side Chain; 3.2.2 A Ring and Its Substitutions; 3.2.3 B Ring and Its Substitutions; 3.2.4 C Ring and Its Substitutions; 3.2.5 D Ring; 3.2.6 Macrocyclic Analogs; 3.2.7 Miscellaneous; 3.3. Exploration on Mechanism of Paclitaxel Related to Tubulin Binding and Quest for Its Pharmacophore3.3.1 Biochemical Mechanism of Paclitaxel Related to Tubulin Binding; 3.3.2 Identification of Bioactive Conformations and Quest for a Pharmacophore for Paclitaxel; 3.4. Natural and Semisynthetic Taxoids Overcoming Multidrug Resistance (MDR); 3.4.1 Structure-Modified Taxoids With Better Activity Toward MDR Tumors; 3.4.2 Nonpaclitaxel-Type Taxoids With MDR Reversal Activities; 3.4.3 Factors Contributing to the Resistance to Paclitaxel; 3.5 Design, Synthesis and Pharmacological Activity of Prodrugs of Paclitaxel3.5.1 Prodrugs Prepared to Improve Water Solubility; 3.5.2 Prodrugs Designed for Enhancing Specificity; 3.6 Other Biological Actions of Paclitaxel; 3.7 New Antimicrotubule Molecules Mimicking Action of Paclitaxel; 3.8 Conclusion; Acknowledgments; References; 4 The Overview of Studies on Huperzine A: A Natural Drug for the Treatment of Alzheimer's Disease; 4.1 Introduction; 4.1.1 Powerful AChEI Originated From Traditional Chinese Medicine; 4.1.2 Alzheimer's Disease; 4.2. Profiles of HA; 4.2.1 Discovery of HA; 4.2.2 Physical Appearance of HA
• Sommario/riassunto: Current discoveries and research into bioactive natural productsMedicinal Chemistry of Bioactive Natural Products provides a much-needed survey of bioactive natural products and their applications in medicinal chemistry. This comprehensive reference features articles by some of the world's leading scientists in the field on discovery, structure elucidation, and elegant synthetic strategies--developed for natural products--with an emphasis on the structure activity relationship of bioactive natural products. The topics have been carefully chosen on the basis of relevance to current rese