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

SL Gwaltney, HM Imade, KJ Barr, Q Li, L Gehrke…

Index: Gwaltney II, Stephen L.; Imade, Hovis M.; Barr, Kenneth J.; Li, Qun; Gehrke, Laura; Credo; Warner, Robert B.; Lee, Jang Yun; Kovar, Peter; Wang, Jieyi; Nukkala, Michael A.; Zielinski, Nicolette A.; Frost, David; Ng, Shi-Chung; Sham, Hing L. Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 7 p. 871 - 874

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Citation Number: 50

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.