Abstract
N-Acetylcolchinol methyl ether 1 served as the starting material to prepare the chloroacetamide (3) and epoxide (5) analogues. Both 3 and 5 were potent inhibitors of tubulin polymerization in vitro. Compound 3 was also 4-fold more cytotoxic than colchicine against the 1A9 tumor cell line and showed a unique cross-resistance profile.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / pharmacology*
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Colchicine / analogs & derivatives*
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Colchicine / chemical synthesis*
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Colchicine / pharmacology*
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Drug Screening Assays, Antitumor
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Humans
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Indicators and Reagents
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Models, Molecular
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Molecular Conformation
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Tubulin / drug effects*
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Tumor Cells, Cultured
Substances
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Antineoplastic Agents
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Indicators and Reagents
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Tubulin
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allocolchicine
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Colchicine