Total synthesis and anti-tubulin activity of Epi-C3 analogues of cryptophycin-24

被引：18

作者：

Buck, SB

Huff, JK

Himes, RH

Georg, GI

机构：

[1] Univ Kansas, Dept Med Chem, Lawrence, KS 66045 USA

[2] Univ Kansas, Dept Mol Biosci, Lawrence, KS 66045 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2004年 / 47卷 / 14期

关键词：

D O I：

10.1021/jm030555f

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Epi-C3-cryptophycin-24, epi-C3-m-chlorobenzyl-cryptophycin-24, and the corresponding styrenes were synthesized and tested in vitro against the MCF-7 and multidrug-resistant MCF-7/ADR breast cancer cell lines and in an in vitro tubulin assembly assay. The results demonstrate that the S configuration at the C3 stereocenter is not required to induce potent cytotoxicity and the m-Cl substituent present on the C10 side chain did not induce any large change in activity.

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收藏

页码：3697 / 3699

页数：3

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