Exploration of the HDAC2 foot pocket: Synthesis and SAR of substituted N-(2-aminophenyl)benzamides.
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Bressi JC, Jennings AJ, Skene R, Wu Y, Melkus R, De Jong R, O'Connell S, Grimshaw CE, Navre M, Gangloff AR
Exploration of the HDAC2 foot pocket: Synthesis and SAR of substituted N-(2-aminophenyl)benzamides.
Bioorg Med Chem Lett. 2010 May 15;20(10):3142-5. doi: 10.1016/j.bmcl.2010.03.091. Epub 2010 Mar 30.
- PubMed ID
- 20392638 [ View in PubMed]
- Abstract
A series of N-(2-amino-5-substituted phenyl)benzamides (3-21) were designed, synthesized and evaluated for their inhibition of HDAC2 and their cytotoxicity in HCT116 cancer cells. Multiple compounds from this series demonstrated time-dependent binding kinetics that is rationalized using a co-complex crystal structure of HDAC2 and N-(4-aminobiphenyl-3-yl)benzamide (6).
DrugBank Data that Cites this Article
- Polypeptides
Name UniProt ID Histone deacetylase 2 Q92769 Details - Binding Properties
Drug Target Property Measurement pH Temperature (°C) Vorinostat Histone deacetylase 2 IC 50 (nM) 72 N/A N/A Details Vorinostat Histone deacetylase 2 IC 50 (nM) 76 N/A N/A Details