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