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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Veröffentlicht in: | British journal of cancer 1995-04, Vol.71 (4), p.705-711 |
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Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | 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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ISSN: | 0007-0920 1532-1827 |
DOI: | 10.1038/bjc.1995.138 |