Abstract
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.
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Woods, J., Hadfield, J., Pettit, G. et al. The interaction with tubulin of a series of stilbenes based on combretastatin A-4. Br J Cancer 71, 705–711 (1995). https://doi.org/10.1038/bjc.1995.138
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DOI: https://doi.org/10.1038/bjc.1995.138
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