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Exploration of the HDAC2 foot pocket: Synthesis and SAR of substituted N-(2-aminophenyl)benzamides

2010; Elsevier BV; Volume: 20; Issue: 10 Linguagem: Inglês

10.1016/j.bmcl.2010.03.091

1464-3405

Jerome C. Bressi, Andy Jennings, R.J. Skene, Yiqin Wu, Robert Melkus, Ron de Jong, Shawn M. O’Connell, Charles E. Grimshaw, Marc Navre, Anthony R. Gangloff,

Protein Degradation and Inhibitors

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).