Design, synthesis and biological studies of novel tubulin inhibitors

Bioorg Med Chem Lett. 2013 Aug 1;23(15):4465-8. doi: 10.1016/j.bmcl.2013.04.078. Epub 2013 May 7.

Abstract

A series of compounds originally derived from the vascular endothelial growth factor receptor tyrosine kinase inhibitor, SU5416, were synthesized and evaluated. The most potent compound in this series, compound 3, which structurally resembles the potent anti-microtubule agent combretastatin A-4, inhibited tubulin polymerization and showed potent growth inhibitory activities on both prostate and breast cancer lines with IC50 values in the low nanomolar range.

Publication types

  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Bibenzyls / pharmacology
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Drug Design*
  • Humans
  • Polymerization / drug effects
  • Tubulin / chemistry
  • Tubulin / metabolism*
  • Tubulin Modulators / chemical synthesis*
  • Tubulin Modulators / chemistry
  • Tubulin Modulators / pharmacology

Substances

  • Antineoplastic Agents
  • Bibenzyls
  • Tubulin
  • Tubulin Modulators
  • combretastatin