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. 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

Pierre Tessier  1 , David V Smil, Amal Wahhab, Silvana Leit, Jubrail Rahil, Zuomei Li, Robert Déziel, Jeffrey M Besterman
Affiliations

Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors

Pierre Tessier et al. Bioorg Med Chem Lett. .

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.

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