（+）- 盘尼西丁的氨基甲酸酯取代类似物的设计、合成与评估。

Design, synthesis, and evaluation of carbamate-substituted analogues of (+)-discodermolide.

作者信息

Smith Amos B, Freeze B Scott, Lamarche Matthew J, Hirose Tomoyasu, Brouard Ignacio, Rucker Paul V, Xian Ming, Sundermann Kurt F, Shaw Simon J, Burlingame Mark A, Horwitz Susan Band, Myles David C

机构信息

Department of Chemistry, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA.

出版信息

Org Lett. 2005 Jan 20;7(2):311-4. doi: 10.1021/ol047686a.

DOI:10.1021/ol047686a

PMID:15646985

Abstract

[Structure: see text] The design, syntheses, and biological evaluation of 22 totally synthetic analogues of the potent microtubule-stabilizing agent (+)-discodermolide (1) have been achieved. Structure-activity relationships of the C(19) carbamate were defined, exploiting two synthetically simplified scaffolds, as well as the parent (+)-discodermolide framework.

摘要

[结构：见正文] 已完成对强效微管稳定剂（+）-盘状海绵内酯（1）的22种全合成类似物的设计、合成及生物学评价。利用两种合成简化的支架以及母体（+）-盘状海绵内酯骨架，确定了C（19）氨基甲酸酯的构效关系。