Arylthioindoles, Potent Inhibitors of Tubulin Polymerization
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- 9 November 2004
- journal article
- letter
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 47 (25) , 6120-6123
- https://doi.org/10.1021/jm049360d
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 IC50 = 2.0 μM, 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 IC50 = 13 nM. Colchicine and CSA4 had 13 nM and 17 nM IC50 values, respectively, with these cells.Keywords
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