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
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
收藏
页码:3507 / 3509
页数:3
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