Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors.

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Tessier P, Smil DV, Wahhab A, Leit S, Rahil J, Li Z, Deziel R, Besterman JM

Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors.

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

PubMed ID
19699639 [ View in PubMed
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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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
VorinostatHistone deacetylase 1IC 50 (nM)140N/AN/ADetails
VorinostatHistone deacetylase 2IC 50 (nM)200N/AN/ADetails