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Bioorg Med Chem Lett. 2009 Feb 1;19(3):688-92. doi: 10.1016/j.bmcl.2008.12.045. Epub 2008 Dec 14.

Novel HDAC6 isoform selective chiral small molecule histone deacetylase inhibitors.

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1
MethylGene Inc, Department of Medicinal Chemistry, 7220 Frederick-Banting, Montréal, Que., Canada H4S 2A1. smild@methylgene.com

Abstract

In an effort to identify HDAC isoform selective inhibitors, we designed and synthesized novel, chiral 3,4-dihydroquinoxalin-2(1H)-one and piperazine-2,5-dione aryl hydroxamates showing selectivity (up to 40-fold) for human HDAC6 over other class I/IIa HDACs. The observed selectivity and potency (IC(50) values 10-200 nM against HDAC6) is markedly dependent on the absolute configuration of the chiral moiety, and suggests new possibilities for use of chiral compounds in selective HDAC isoform inhibition.

PMID:
19111466
DOI:
10.1016/j.bmcl.2008.12.045
[Indexed for MEDLINE]
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