The interaction with tubulin of a series of stilbenes based on combretastatin A-4

TY - JOUR

T1 - The interaction with tubulin of a series of stilbenes based on combretastatin A-4

AU - Woods, J. A.

AU - Hadfield, J. A.

AU - Pettit, G. R.

AU - Fox, B. W.

AU - McGown, A. T.

PY - 1995/4

Y1 - 1995/4

N2 - 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.

AB - 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.

KW - Tubulin

KW - Combrestatins

KW - Structure-activity

U2 - 10.1038/bjc.1995.138

DO - 10.1038/bjc.1995.138

M3 - Article

C2 - 7710932

SN - 0007-0920

VL - 71

SP - 705

EP - 711

JO - British Journal of Cancer

JF - British Journal of Cancer

IS - 4

ER -