Effects of the hydrophobicity of taxoids on their interaction with tubulin

被引：18

作者：

Guénard, D ^{[1
]}

Thoret, S ^{[1
]}

Dubois, J ^{[1
]}

Adeline, MT ^{[1
]}

Wang, Q ^{[1
]}

Guéritte, F ^{[1
]}

机构：

[1] CNRS, Inst Chim Subst Nat, F-91190 Gif Sur Yvette, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2000年 / 8卷 / 01期

关键词：

docetaxel tubulin; hydrophobicity; structure-activity relationships;

D O I：

10.1016/S0968-0896(99)00279-5

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Modifications of the hydrophobic character at the 7 and 10 positions of the taxoids greatly modified the effect of these drugs on the tubulin-microtubule system. The presence of an alkyl chain at these positions decreased the activity while their corresponding more polar analogues restored the activity of these molecules. It appears that the recognition of taxoids by tubulin depends on the location of the most important hydrophobic area. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：145 / 156

页数：12

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