Identification of novel HDAC inhibitors through cell based screening and their evaluation as potential anticancer agents

  • Bioorg Med Chem Lett. 2013 Sep 1;23(17):4790-3. doi: 10.1016/j.bmcl.2013.07.001.
Tong Wang  1 ,  Mario Sepulveda ,  Paul Gonzales ,  Stephen Gately
Affiliations
  • 1. Translational Drug Development, Inc, 13208 E Shea Boulevard, Suite 100, Scottsdale, AZ 85259,USA. [email protected]
PMID: 23906422 DOI: 10.1016/j.bmcl.2013.07.001
Abstract

A series of benzimidazole based HDAC inhibitors have been rationally designed, synthesized and screened. The SAR of this new chemotype is described. The lead compound, 11e, showed strong activity in several cellular assays and demonstrated in vivo efficacy in mouse xenograft pancreatic Cancer models.

Keywords
Anticancer agents; Benzimidazole; HDAC inhibitors; Structure–activity relationship.