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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 ORCID:, 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: 05 Jan 2024 05:58

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