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  • Arylthioindoles, Potent Inh...
    De Martino, Gabriella; La Regina, Giuseppe; Coluccia, Antonio; Edler, Michael C; Barbera, Maria Chiara; Brancale, Andrea; Wilcox, Elizabeth; Hamel, Ernest; Artico, Marino; Silvestri, Romano

    Journal of medicinal chemistry, 12/2004, Letnik: 47, Številka: 25
    Journal Article

    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 μM, 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.