Abstract
Several arylthioindoles had excellent activity as inhibitors both of tubulin polymerization and of the growth of MCF-7 human breast carcinoma cells. Methyl 3-[(3,4,5-trimethoxyphenyl)thio]-5-methoxy-1H-indole-2-carboxylate (21), the most potent derivative, showed IC(50) = 2.0 microM, 1.6 times more active than colchicine and about as active as combretastatin A-4 (CSA4). Compound 21 inhibited the growth of the MCF-7 cells at IC(50) = 13 nM. Colchicine and CSA4 had 13 nM and 17 nM IC(50) values, respectively, with these cells.
MeSH terms
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology
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Biopolymers
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Cell Line, Tumor
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Crystallography, X-Ray
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Depression, Chemical
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Drug Screening Assays, Antitumor
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Humans
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Indoles / chemical synthesis*
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Indoles / chemistry
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Indoles / pharmacology
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Models, Molecular
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Sulfides / chemical synthesis*
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Sulfides / chemistry
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Sulfides / pharmacology
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Tubulin / chemistry*
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Tubulin Modulators*
Substances
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Antineoplastic Agents
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Biopolymers
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Indoles
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Sulfides
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Tubulin
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Tubulin Modulators