Synthesis and biological evaluation of piperamide analogues as HDAC inhibitors

  • Bioorg Med Chem Lett. 2011 Aug 15;21(16):4844-6. doi: 10.1016/j.bmcl.2011.06.046.
Yu Luo  1 ,  Hao-Min Liu ,  Ming-Bo Su ,  Li Sheng ,  Yu-Bo Zhou ,  Jia Li ,  Wei Lu
Affiliations
  • 1. Department of Chemistry, East China Normal University, 3663 North Zhongshan Road, Shanghai 200062, PR China.
PMID: 21745740 DOI: 10.1016/j.bmcl.2011.06.046
Abstract

Two natural piperamides (piperlonguminine and refrofractamide A) and their derivatives were synthesized and evaluated for inhibitory activity against histone deacetylases, as well as the HCT-116 human colon Cancer cell line. The preliminary structure activity relationship was discussed. Compounds featuring a hydroxamic acid moiety exhibited moderate HDAC activity and in vitro cytotoxicity.