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

Br J Cancer. 1995 Apr;71(4):705-11. doi: 10.1038/bjc.1995.138.


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.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents, Phytogenic / chemistry*
  • Antineoplastic Agents, Phytogenic / toxicity
  • Binding, Competitive
  • Cell Cycle / drug effects
  • Leukemia P388
  • Mice
  • Microtubules / drug effects
  • Microtubules / ultrastructure*
  • Mitotic Index / drug effects
  • Molecular Structure
  • Stilbenes / chemical synthesis
  • Stilbenes / chemistry*
  • Stilbenes / toxicity
  • Structure-Activity Relationship
  • Thermodynamics
  • Tubulin / chemistry*
  • Tumor Cells, Cultured


  • Antineoplastic Agents, Phytogenic
  • Stilbenes
  • Tubulin
  • fosbretabulin