doi: 10.1021/jm049360d.
Arylthioindoles, potent inhibitors of tubulin polymerization
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- PMID: 15566282
- DOI: 10.1021/jm049360d
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Arylthioindoles, potent inhibitors of tubulin polymerization
J Med Chem.
.
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.
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