Design and synthesis of a novel class of histone deacetylase inhibitors

被引：75

作者：

Lavoie, R

Bouchain, G

Frechette, S

Woo, SH

Abou Khalil, E

Leit, S

Fournel, M

Yan, PT

Trachy-Bourget, MC

Beaulieu, C

Li, ZM

Besterman, J

Delorme, D

机构：

[1] MethylGene Inc, Dept Med Chem, Montreal, PQ H4S 2A1, Canada

[2] MethylGene Inc, Dept Biol, Montreal, PQ H4S 2A1, Canada

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 21期

关键词：

D O I：

10.1016/S0960-894X(01)00552-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Histone deacetylase inhibitors (HDACs) have emerged as a novel class of antiproliferative agents. Utilizing structure-based design, the synthesis of a series of sulfonamide hydroxamic acids is described. Further optimization of this series by substitution of the terminal aromatic ring yielded HDAC inhibitors with good in vitro and in vivo activities. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：2847 / 2850

页数：4

共 19 条

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[2]

Butler LM, 2000, CANCER RES, V60, P5165

[3] HDA1 and HDA3 are components of a yeast histone deacetylase (HDA) complex [J].