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

J. A. Woods, J. A. Hadfield, G. R. Pettit, B. W. Fox, A. T. McGown

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    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.
    Original languageEnglish
    Pages (from-to)705-11
    Number of pages7
    JournalBritish Journal of Cancer
    Volume71
    Issue number4
    DOIs
    Publication statusPublished - Apr 1995

    Keywords

    • Tubulin
    • Combrestatins
    • Structure-activity

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    Woods, J. A., Hadfield, J. A., Pettit, G. R., Fox, B. W., & McGown, A. T. (1995). The interaction with tubulin of a series of stilbenes based on combretastatin A-4. British Journal of Cancer, 71(4), 705-11. https://doi.org/10.1038/bjc.1995.138