Novel sulfonate analogues of combretastatin A-4: potent antimitotic agents

Bioorg Med Chem Lett. 2001 Apr 9;11(7):871-4. doi: 10.1016/s0960-894x(01)00098-1.

Abstract

Sulfonate analogues of combretastatin A-4 have been prepared. These compounds compete with colchicine and combretastatin A-4 for the colchicine binding site on tubulin and are potent inhibitors of tubulin polymerization and cell proliferation. Importantly, these compounds also inhibit the proliferation of P-glycoprotein positive (+) cancer cells, which are resistant to many other antitumor agents.

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / biosynthesis
  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / genetics
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Binding Sites / physiology
  • Binding, Competitive
  • Cell Division / drug effects
  • Colchicine / antagonists & inhibitors*
  • Colchicine / metabolism
  • Humans
  • Polymers / metabolism
  • Stilbenes / chemistry*
  • Stilbenes / pharmacology*
  • Tubulin / metabolism
  • Tubulin Modulators*
  • Tumor Cells, Cultured / cytology
  • Tumor Cells, Cultured / drug effects

Substances

  • ATP Binding Cassette Transporter, Subfamily B, Member 1
  • Antineoplastic Agents
  • Polymers
  • Stilbenes
  • Tubulin
  • Tubulin Modulators
  • fosbretabulin
  • Colchicine