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

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'-...

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Detalles Bibliográficos
Autores principales: Woods, J. A., Hadfield, J. A., Pettit, G. R., Fox, B. W., McGown, A. T.
Formato: Texto
Lenguaje:English
Publicado: Nature Publishing Group 1995
Materias:
Research Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2033763/
https://www.ncbi.nlm.nih.gov/pubmed/7710932
Descripción
Sumario: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. IMAGES:

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