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Bioorg Med Chem Lett. 2007 Jan 1;17(1):136-41. Epub 2006 Sep 30.

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

Author information

1
Department of Chemistry, University College London, Christopher Ingold Laboratories, 20 Gordon Street, London WC1H OAJ, UK. c.m.marson@ucl.ac.uk

Abstract

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 (IC(50)=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 IC(50) values down to 1 nM being obtained.

PMID:
17046252
DOI:
10.1016/j.bmcl.2006.09.085
[Indexed for MEDLINE]

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