Abstract
The bifunctional taxoid-colchicinoid hybrids 6-8 were synthesized and evaluated in assays of cytotoxicity and tubulin assembly/disassembly. All compounds showed a high degree of cytotoxicity, but, while 6 and 7 behaved as bifunctional tubulin binders not unlike an equimolecular mixture of taxol and thiocolchicine, 8 was surprisingly devoid of tubulin activity, acting on a distinct and yet to identify molecular target.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antineoplastic Combined Chemotherapy Protocols* / chemical synthesis
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Antineoplastic Combined Chemotherapy Protocols* / pharmacology
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Cattle
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Cell Line, Tumor
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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 / methods
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Humans
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Microtubules / drug effects
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Microtubules / physiology
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Paclitaxel / chemical synthesis*
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Paclitaxel / pharmacology*
Substances
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thiocholchicine
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Paclitaxel
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Colchicine