Synthesis and biological evaluation of A-ring biaryl-carbamate analogues of rhazinilam

被引：35

作者：

Baudoin, O ^{[1
]}

Claveau, F ^{[1
]}

Thoret, S ^{[1
]}

Herrbach, A ^{[1
]}

Guénard, D ^{[1
]}

Guéritte, F ^{[1
]}

机构：

[1] CNRS, Inst Chim Subst Nat, F-91198 Gif Sur Yvette, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2002年 / 10卷 / 11期

关键词：

D O I：

10.1016/S0968-0896(02)00270-5

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：

An improvement of the synthesis of biphenyl-carba mate 2a, the most active analogue of rhazinilam 1 so far, was performed using the Pd-catalyzed borylation/Suzuki coupling (BSC) method developed in our laboratories. The preparation of A-ring analogues of 2a bearing electron-withdrawing or donating groups is reported according to this new synthetic scheme. The anti-tubulin properties as well as the cytotoxicity of these compounds toward human cancer cell lines were evaluated in comparison with rhazinilam and 2a. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：3395 / 3400

页数：6

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