Aminosuberoyl hydroxamic acids (ASHAs): A potent new class of HDAC inhibitors

被引：31

作者：

Belvedere, Sandro

Witter, David J.

Yan, Jiaming

Secrist, J. Paul

Richon, Victoria

Miller, Thomas A.

机构：

[1] Merck Res Labs, Dept Drug Design & Optimizat, Boston, MA 02115 USA

[2] Merck Res Labs, Dept Canc & Biol Therapeut, Boston, MA 02115 USA

[3] ARMGO Pharma Inc, New York, NY 10032 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 14期

关键词：

HDAC; histone deacetylase inhibitor; HDAC inhibitor; anticancer drug; SAHA; hydroxamic acids;

D O I：

10.1016/j.bmcl.2007.04.089

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Histone deacetylase (HDAC) inhibitors that target Class I and Class II HDACs are currently in advanced clinical trials for the treatment of cancer. Vorinostat (Zolinza (TM), SAHA) is a hydroxamic acid approved for the treatment of patients with cutaneous T-cell lymphoma who have progressive, persistent or recurrent disease on or following two systemic therapies. As part of an on-going effort to better understand the nature of the HDAC enzyme/inhibitor interaction and design highly effective HDAC inhibitors, we herein report the design, synthesis and HDAC inhibitory activity of a vorinostat-derived series of substrate-based HDAC inhibitors. (C) 2007 Elsevier Ltd. All rights reserved.

引用

页码：3969 / 3971

页数：3

共 12 条

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