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Arylthioindoles, potent inhibitors of tubulin polymerization

De Martino, Gabriella, La Regina, Giuseppe, Coluccia, Antonio, Edler, Michael C., Barbera, Maria Chiara, Brancale, Andrea, Wilcox, Elizabeth, Hamel, Ernest, Artico, Marino and Silvestri, Romano 2004. Arylthioindoles, potent inhibitors of tubulin polymerization. Journal of Medicinal Chemistry 47 (25) , pp. 6120-6123. 10.1021/jm049360d

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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 íM, 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.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Pharmacy
Subjects: R Medicine > RS Pharmacy and materia medica
ISSN: 0022-2623
Last Modified: 04 Jun 2017 02:00

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