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

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.
Jerome C Bressi 1,  Andy J Jennings,  Robert Skene,  Yiqin Wu,  Robert Melkus,  Ron De Jong,  Shawn O'Connell,  Charles E Grimshaw,  Marc Navre,  Anthony R Gangloff
Affiliations

Affiliation

  • 1 Takeda San Diego, San Diego, CA 92121, USA.
PMID: 20392638 DOI: 10.1016/j.bmcl.2010.03.091
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).

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