De Martino Gabriella, La Regina Giuseppe, Coluccia Antonio, Edler Michael C, Barbera Maria Chiara, Brancale Andrea, Wilcox Elizabeth, Hamel Ernest, Artico Marino, Silvestri Romano
Dipartimento di Studi Farmaceutici, Università di Roma, La Sapienza, I-00185 Rome, Italy.
J Med Chem. 2004 Dec 2;47(25):6120-3. doi: 10.1021/jm049360d.
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.
几种芳硫基吲哚作为微管蛋白聚合抑制剂和MCF-7人乳腺癌细胞生长抑制剂均具有优异的活性。最有效的衍生物3-[(3,4,5-三甲氧基苯基)硫代]-5-甲氧基-1H-吲哚-2-羧酸甲酯（21）的IC(50) = 2.0 μM，活性是秋水仙碱的1.6倍，与康普瑞他汀A-4（CSA4）活性相当。化合物21在IC(50) = 13 nM时可抑制MCF-7细胞的生长。秋水仙碱和CSA4对这些细胞的IC(50)值分别为13 nM和17 nM。
