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Bioorg Med Chem Lett. 2009 Oct 1;19(19):5684-8. doi: 10.1016/j.bmcl.2009.08.010. Epub 2009 Aug 7.

Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors.

Author information

1
MethylGene Inc., Department of Medicinal Chemistry, 7220 Frederick-Banting, Montréal, Québec, Canada H4S 2A1.

Abstract

We have identified a series of diphenylmethylene hydroxamic acids as novel and selective HDAC class IIa inhibitors. The original hit, N-hydroxy-2,2-diphenylacetamide (6), has sub-micromolar class IIa HDAC inhibitory activity, while the rigidified oxygen analogue, N-hydroxy-9H-xanthene-9-carboxamide (13), is slightly more selective for HDAC7 with an IC(50) of 0.05muM. Substitution of 6 allows for the modulation of selectivity and potency amongst the class IIa HDAC isotypes.

PMID:
19699639
DOI:
10.1016/j.bmcl.2009.08.010
[Indexed for MEDLINE]

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