Arylthioindoles, potent inhibitors of tubulin polymerization

  • J Med Chem. 2004 Dec 2;47(25):6120-3. doi: 10.1021/jm049360d.
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
Affiliations
  • 1. Dipartimento di Studi Farmaceutici, Università di Roma, La Sapienza, I-00185 Rome, Italy.
PMID: 15566282 DOI: 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 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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