Sulfonate analogues of combretastatin A-4 have been prepared. These compoun
ds compete with colchicine and combretastatin A-4 for the colchicine bindin
g site on tubulin and are potent inhibitors of tubulin polymerization and c
ell proliferation. Importantly, these compounds also inhibit the proliferat
ion of P-glycoprotein positive (+) cancer cells, which are resistant to man
y other antitumor agents. (C) 2001 Elsevier Science Ltd. All rights reserve
d.