Structure-activity relationships of aryloxyalkanoic acid hydroxyamides as potent inhibitors of histone deacetylase

被引：17
作者：
Marson, Charles M.
Mahadevan, Thevaki
Dines, Jon
Sengmany, Stphane
Morrell, James M.
Alao, John P.
Joel, Simon P.
Vigushin, David M.
Coombes, R. Charles
机构：
[1] UCL, Christopher Ingold Labs, Dept Chem, London WC1H 0AJ, England
[2] Imperial Coll Sch Med, Dept Canc Med, London W12 0NN, England
[3] St Bartholomews Hosp, Inst Canc, Ctr Med Oncol, London EC1A 7BE, England
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 01期
基金：
英国生物技术与生命科学研究理事会; 英国工程与自然科学研究理事会;
关键词：
histone deacetylase; enzyme inhibitors; hydroxamic acids; aryloxyalkanoic acid derivatives;
D O I：
10.1016/j.bmcl.2006.09.085
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Syntheses of aryloxyalkanoic acid hydroxyamides are described, all of which are potent inhibitors of histone deacetylase, some being more potent in vitro than trichostatin A (IC50 = 3 nM). Variation of the substituents on the benzene ring as well as fusion of a second ring have marked effects on potency, in vitro IC50 values down to I nM being obtained. (c) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码：136 / 141
页数：6
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