Abstract
A new trifluorinated amino-combretastatin analogue, (Z)-2-(4'-methoxy-3'-aminophenyl)-1-(3,4,5-trifluorophenyl)ethene, prepared by chemical synthesis, was found to be a potent inhibitor of tubulin assembly (IC(50)=2.9 microM), and cytotoxic against selected human cancer cell lines. This new lead compound is among the most active from a group of related structural modifications.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Antineoplastic Agents, Phytogenic / chemical synthesis*
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Antineoplastic Agents, Phytogenic / chemistry
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Antineoplastic Agents, Phytogenic / pharmacology*
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Bibenzyls / chemical synthesis*
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Bibenzyls / chemistry
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Bibenzyls / pharmacology*
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Combinatorial Chemistry Techniques
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Drug Design*
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Drug Screening Assays, Antitumor
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Humans
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Hydrocarbons, Fluorinated / chemical synthesis*
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Hydrocarbons, Fluorinated / chemistry
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Hydrocarbons, Fluorinated / pharmacology*
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Inhibitory Concentration 50
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Molecular Structure
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Stereoisomerism
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Stilbenes / chemistry*
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Stilbenes / pharmacology*
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Structure-Activity Relationship
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Tubulin / metabolism*
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Tubulin Modulators / pharmacology*
Substances
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(Z)-2-(4'-methoxy-3'-aminophenyl)-1-(3,4,5-trifluorophenyl)ethene
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Antineoplastic Agents, Phytogenic
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Bibenzyls
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Hydrocarbons, Fluorinated
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Stilbenes
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Tubulin
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Tubulin Modulators
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fosbretabulin