2. Academic Validation
  3. Synthesis and biological evaluation of piperamide analogues as HDAC inhibitors

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

Affiliation

  • 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.

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