Indole amide hydroxamic acids as potent inhibitors of histone deacetylases

被引：51

作者：

Dai, YJ ^{[1
]}

Guo, Y ^{[1
]}

Guo, J ^{[1
]}

Pease, LJ ^{[1
]}

Li, JL ^{[1
]}

Marcotte, PA ^{[1
]}

Glaser, KB ^{[1
]}

Tapang, P ^{[1
]}

Albert, DH ^{[1
]}

Richardson, PL ^{[1
]}

Davidsen, SK ^{[1
]}

Michaelides, MR ^{[1
]}

机构：

[1] Abbott Labs, Canc Res, Dept R47J, Abbott Pk, IL 60064 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 11期

关键词：

D O I：

10.1016/S0960-894X(03)00301-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of hydroxamic acid-based HDAC inhibitors with an indole amide residue at the terminus have been synthesized and evaluated. Compounds with a 2-indole amide moiety have been found as the most active inhibitors among the different regioisomers. Introduction of substituents on the indole ring further improved the potency and generated a series of very potent inhibitors with significant antiproliferative activity. A representative compound in the series, 7b, has been found to be orally active in tumor growth inhibition model. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：1897 / 1901

页数：5

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