Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors.
Article Details
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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]
- 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
Drug Target Property Measurement pH Temperature (°C) Vorinostat Histone deacetylase 1 IC 50 (nM) 140 N/A N/A Details Vorinostat Histone deacetylase 2 IC 50 (nM) 200 N/A N/A Details