（+）-软海绵素简化类似物的设计、合成及生物学评价。关于二烯、C7羟基和内酯重要性的更多见解。

Design, synthesis, and biological evaluation of simplified analogues of (+)-discodermolide. Additional insights on the importance of the diene, the C7 hydroxyl, and the lactone.

作者信息

Smith Amos B, Xian Ming

机构信息

Department of Chemistry, Monell Chemical Senses Center, and Laboratory for Research on the Structure of Matter, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA.

出版信息

Org Lett. 2005 Nov 10;7(23):5229-32. doi: 10.1021/ol052070m.

DOI:10.1021/ol052070m

PMID:16268545

Abstract

[structure: see text] The design, synthesis, and biological evaluation of seven totally synthetic analogues of the antitumor agent (+)-discodermolide are reported. Saturation of the terminal diene system, alteration of the substituents on the lactone, and alkylation of the C7-hydroxyl group reveal significant structure-activity relationships.

摘要

[结构：见正文] 报道了抗肿瘤药物(+)-盘状海绵内酯的七种全合成类似物的设计、合成及生物学评价。末端二烯系统的饱和、内酯上取代基的改变以及C7-羟基的烷基化揭示了显著的构效关系。