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. 2004 Dec 2;47(25):6120-3.
doi: 10.1021/jm049360d.

Arylthioindoles, potent inhibitors of tubulin polymerization (V体育2025版)

Gabriella De Martino  1 , Giuseppe La Regina, Antonio Coluccia, Michael C Edler, Maria Chiara Barbera, Andrea Brancale, Elizabeth Wilcox, Ernest Hamel, Marino Artico, Romano Silvestri
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Arylthioindoles, potent inhibitors of tubulin polymerization

Gabriella De Martino et al. 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. VSports手机版.

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