埃坡霉素的化学生物学

Chemical Biology of Epothilones.

作者信息

Nicolaou K C, Roschangar Frank, Vourloumis Dionisios

机构信息

Department of Chemistry and, The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037 (USA), Fax: (+1) 619-784-2469 (and) Department of Chemistry and Biochemistry, University of California, San Diego, 9500 Gilman Drive, La Jolla, California 92093 (USA).

出版信息

Angew Chem Int Ed Engl. 1998 Aug 17;37(15):2014-2045. doi: 10.1002/(SICI)1521-3773(19980817)37:15<2014::AID-ANIE2014>3.0.CO;2-2.

DOI:10.1002/(SICI)1521-3773(19980817)37:15<2014::AID-ANIE2014>3.0.CO;2-2

PMID:29711063

Abstract

Only a few months after the disclosure of the absolute configuration of epothilones A (R=H, see picture on the right) and B (R=Me) the first total syntheses of these natural products were reported. Interest intensified with the realization of their potential as anticancer agents with a taxol-like mechanism of action. In addition to describing the most important total syntheses and biological properties of the naturally occurring epothilones A-E, this review also provides a systematic overview of numerous epothilone analogues that have been modified in the A-D regions in order to obtain information about structure-activity relationships.

摘要

在埃坡霉素A（R = H，见右图）和B（R = Me）的绝对构型被披露仅几个月后，就有了关于这些天然产物的首次全合成报道。随着人们认识到它们作为具有类似紫杉醇作用机制的抗癌剂的潜力，兴趣日益浓厚。除了描述天然存在的埃坡霉素A - E的最重要全合成和生物学特性外，本综述还对在A - D区域进行了修饰的众多埃坡霉素类似物进行了系统概述，以便获得有关构效关系的信息。