Structure-activity relationships within a family of selectively cytotoxic macrolide natural products

被引：44

作者：

Salomon, AR ^{[1
]}

Zhang, YB

Seto, H

Khosla, C

机构：

[1] Stanford Univ, Dept Chem, Stanford, CA 94305 USA

[2] Stanford Univ, Dept Chem Engn, Stanford, CA 94305 USA

来源：

ORGANIC LETTERS | 2001年 / 3卷 / 01期

关键词：

D O I：

10.1021/ol006767d

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

[GRAPHICS] We describe a semi-synthetic deglycosylated derivative of apoptolidin that retains considerable activity against the mitochondrial ATPase but has greatly reduced cellular cytotoxicity. We also demonstrate that a related antifungal natural product, cytovaricin, inhibits the same molecular target. Structural comparison of these macrolides provides insights into their conserved features that are presumably important for biological activity and identifies promising avenues at the interface of organic synthesis and biosynthesis for the generation of new selective cytotoxic agents.

引用

页码：57 / 59

页数：3

共 10 条

[1]

FERRIER RJ, 1968, J CHEM SOC C, P947

[2] AMINO-ACID SUBSTITUTIONS IN MITOCHONDRIAL ATP SYNTHASE SUBUNIT-9 OF SACCHAROMYCES-CEREVISIAE LEADING TO VENTURICIDIN OR OSSAMYCIN RESISTANCE [J].