Arylthioindoles, potent inhibitors of tubulin polymerization

被引：277

作者：

De Martino, G

La Regina, G

Coluccia, A

Edler, MC

Barbera, MC

Brancale, A

Wilcox, E

Hamel, E

Artico, M

Silvestri, R

机构：

[1] Univ Roma La Sapienza, Dipartimento Studi Farmaceut, I-00185 Rome, Italy

[2] Cardiff Univ, Welsh Sch Pharm, Cardiff CF10 3XF, S Glam, Wales

[3] NCI, Screening Technol Branch, Dev Therapeut Program, Div Canc Treatment & Diag,NIH, Frederick, MD 21702 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2004年 / 47卷 / 25期

关键词：

D O I：

10.1021/jm049360d

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 muM, 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.

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页码：6120 / 6123

页数：4

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