Conformationally restricted paclitaxel analogues: Macrocyclic mimics of the "hydrophobic collapse" conformation

被引：40

作者：

Boge, TC

Wu, ZJ

Himes, RH

Vander Velde, DG

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：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 20期

关键词：

D O I：

10.1016/S0960-894X(99)00522-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Conformationally restricted macrocyclic analogues of paclitaxel were prepared, by connecting the 3'-phenyl group and the 2-benzoate moiety with two-atom tethers to mimic the "hydrophobic collapse" paclitaxel conformation. The analogues did not show activity in a tubulin assembly assay. (C) 1999 Elsevier Science Ltd. All rights reserved.

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页码：3047 / 3052

页数：6

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