Structural requirements for the interaction of combretastatins with tubulin: how important is the trimethoxy unit?

被引：125

作者：

Gaukroger, K

Hadfield, JA

Lawrence, NJ

Nolan, S

McGown, AT

机构：

[1] Christie Hosp NHS Trust, Paterson Inst Canc Res, Drug Dev Sect, Manchester M20 4BX, Lancs, England

[2] Univ Salford, Ctr Mol Drug Design, Salford M5 4WT, Lancs, England

[3] Univ Manchester, Dept Chem, Manchester M60 1QD, Lancs, England

[4] Cardiff Univ, Dept Chem, Cardiff CF10 3TB, S Glam, Wales

来源：

ORGANIC & BIOMOLECULAR CHEMISTRY | 2003年 / 1卷 / 17期

关键词：

D O I：

10.1039/b306878a

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A series of combretastatins possessing both a trimethoxy unit and other substituents on ring A has been synthesised and tested for cytotoxicity and their ability to interact with the protein tubulin. All previous studies have indicated that the trimethoxy unit is essential for interaction with tubulin. The studies herein show that molecules possessing functionalities other than trimethoxy can also interact with tubulin. Importantly a trimethyl substituted agent 52a has shown reduced cytotoxicity, but increased potency in its ability to inhibit the assembly of tubulin.

引用

页码：3033 / 3037

页数：5

共 22 条

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