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.
S L Gwaltney 2nd  1 ,  H M Imade ,  K J Barr ,  Q Li ,  L Gehrke ,  R B Credo ,  R B Warner ,  J Y Lee ,  P Kovar ,  J Wang ,  M A Nukkala ,  N A Zielinski ,  D Frost ,  S C Ng ,  H L Sham
Affiliations
  • 1. Cancer Research, Abbott Laboratories, Abbott Park, IL 60064-6101, USA. [email protected]
PMID: 11294380 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.