جزییات کتاب
Diversity-oriented synthesis is a new paradigm for developing large collections of structurally diverse small molecules as probes to investigate biological pathways. This book presents the most effective methods in diversity-oriented synthesis for creating small molecule collections. It offers tested and proven strategies for developing diversity-oriented synthetic libraries and screening methods for identifying ligands. Lastly, it explores some promising new applications based on diversity-oriented synthesis that have the potential to dramatically advance studies in drug discovery and chemical biology. Diversity-Oriented Synthesis begins with an introductory chapter that explores the basics, including a discussion of the relationship between diversity-oriented synthesis and classic combinatorial chemistry. Divided into four parts, the book: Offers key chemical methods for the generation of small molecules using diversity-oriented principles, including peptidomimetics and macrocycles Expands on the concept of diversity-oriented synthesis by describing chemical libraries Provides modern approaches to screening diversity-oriented synthetic libraries, including high-throughput and high-content screening, small molecule microarrays, and smart screening assays Presents the applications of diversity-oriented synthetic libraries and small molecules in drug discovery and chemical biology, reporting the results of key studies and forecasting the role of diversity-oriented synthesis in future biomedical research This book has been written and edited by leading international experts in organic synthesis and its applications. Their contributions are based on a thorough review of the current literature as well as their own firsthand experience developing synthetic methods and applications. Clearly written and extensively referenced, Diversity-Oriented Synthesis introduces novices to this highly promising field of research and serves as a springboard for experts to advance their own research studies and develop new applications. Content: Chapter 1 The Basics of Diversity?Oriented Synthesis (pages 1–26): Kieron M. G. O'Connell, Warren R. J. D. Galloway and David R. SpringChapter 2 Strategic Applications of Multicomponent Reactions in Diversity?Oriented Synthesis (pages 27–57): John M. Knapp, Mark J. Kurth, Jared T. Shaw and Ashkaan YounaiChapter 3 Cycloaddition reactions in Diversity?Oriented Synthesis (pages 59–95): Giovanni MuncipintoChapter 4 Phosphine Organocatalysis as a Platform for Diversity?Oriented Synthesis (pages 97–133): Zhiming Wang and Ohyun KwonChapter 5 Domino Reactions in Library Synthesis (pages 135–176): Matthew G. LaPorte, John R. Goodell, Sammi Tsegay and Peter WipfChapter 6 Diversity?Oriented Synthesis of Amino Acid–Derived Scaffolds and Peptidomimetics: A Perspective (pages 177–200): Andrea TrabocchiChapter 7 Solid?Phase Synthesis Enabling Chemical Diversity (pages 201–252): Nadezda Cankarova and Viktor KrchnakChapter 8 Macrocycles as Templates for Diversity Generation in Drug Discovery (pages 253–287): Eric MarsaultChapter 9 Diversity?Oriented Synthesis of Natural Product–Like Libraries (pages 289–323): Mark Dow, Francesco Marchetti and Adam NelsonChapter 10 Chemoinformatic Characterization of the Chemical Space and Molecular Diversity of Compound Libraries (pages 325–352): Jose Luis Medina?FrancoChapter 11 DNA?encoded Chemical Libraries (pages 353–399): Luca MannocciChapter 12 Experimental Approaches to Rapid Identification, Profiling, and Characterization of Specific Biological Effects of DOS Compounds (pages 401–429): Eduard A. Sergienko and Susanne Heynen?GenelChapter 13 Small?Molecule Microarrays (pages 431–454): Hongyan SunChapter 14 Yeast as a Model in High?Throughput Screening of Small?Molecule Libraries (pages 455–482): Irene Stefanini, Carlotta De Filippo and Duccio CavalieriChapter 15 Virtual Screening Methods (pages 483–505): Jurgen BajorathChapter 16 Structure–Activity Relationship Data Analysis: Activity Landscapes and Activity Cliffs (pages 507–531): Jurgen BajorathChapter 17 Diversity?Oriented Synthesis and Drug Development: Facilitating the Discovery of Novel Probes and Therapeutics (pages 533–574): Jeremy R. Duvall, Eamon Comer and Sivaraman DandapaniChapter 18 DOS?Derived Small?Molecule Probes in Chemical Biology (pages 575–617): Nicholas Hill, Lingyan Du and Qiu Wang