THE INTERACTION WITH TUBULIN OF A SERIES OF STILBENES BASED ON COMBRETASTATIN A-4

被引：165

作者：

WOODS, JA

HADFIELD, JA

PETTIT, GR

FOX, BW

MCGOWN, AT

机构：

[1] CHRISTIE HOSP & HOLT RADIUM INST,PATERSON INST CANC RES,DEPT EXPTL CHEMOTHERAPY,CRC,MANCHESTER M20 9BX,LANCS,ENGLAND

[2] ARIZONA STATE UNIV,CANC RES INST,TEMPE,AZ 85287

[3] ARIZONA STATE UNIV,DEPT CHEM,TEMPE,AZ 85287

来源：

BRITISH JOURNAL OF CANCER | 1995年 / 71卷 / 04期

关键词：

TUBULIN; COMBRESTATINS; STRUCTURE-ACTIVITY;

D O I：

10.1038/bjc.1995.138

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

A series of stilbenes, based on combretastatin A-4, were synthesised. A structure-activity study was carried out to characterise the interaction of these agents with tubulin. The substitution of small alkyl substituents for the 4'-methoxy group of combretastatin A-4 and the loss of the 3'-hydroxyl group does not have a major effect on the interaction with tubulin. trans-Stilbenes were shown to bind tubulin, but do not inhibit microtubule assembly. This work, together with previous studies, has been used to propose an idealised structure for a tubulin-binding agent of this type.

引用

页码：705 / 711

页数：7