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 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 IC50 ) 13 nanoM. Colchicine and CSA4 had 13 nanoM and 17 nanoM IC50 values, respectively, with these cells.
Arylthioindoles, potent inhibitors of tubulin polymerization / DE MARTINO, G.; LA REGINA, Giuseppe; Coluccia, Antonio; Edler, M. C.; Barbera, M. C.; Brancale, A.; Wilcox, E.; Hamel, E.; Artico, Marino; Silvestri, Romano. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - 47:25(2004), pp. 6120-6123. [10.1021/jm049360d]
Arylthioindoles, potent inhibitors of tubulin polymerization.
LA REGINA, GIUSEPPE;COLUCCIA, Antonio;ARTICO, Marino;SILVESTRI, Romano
2004
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 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 IC50 ) 13 nanoM. Colchicine and CSA4 had 13 nanoM and 17 nanoM IC50 values, respectively, with these cells.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
