Synthesis and biological evaluation of (-)-laulimalide analogues

被引：45

作者：

Wender, PA ^{[1
]}

Hegde, SG

Hubbard, RD

Zhang, L

Mooberry, SL

机构：

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

[2] SW Fdn Biomed Res, Dept Physiol & Med, San Antonio, TX 78245 USA

来源：

ORGANIC LETTERS | 2003年 / 5卷 / 19期

关键词：

D O I：

10.1021/ol035339f

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

[GRAPHICS] The syntheses of five laulimalide analogues are described, incorporating modifications at the C-16-C-17-epoxide, the C-20-alcohol, as well as the C-1-C-3-enoate of the parent natural product. The resultant analogues are active in drug-sensitive HeLa and MDA-MB-435 cell lines. Significantly, like laulimalide, these analogues are poor substrates for the drug transport protein P-glycoprotein (Pgp) and are thus effective against Taxol-resistant cell lines.

引用

页码：3507 / 3509

页数：3

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