Synthesis and biological evaluation of piperamide analogues as HDAC inhibitors

Y Luo, HM Liu, MB Su, L Sheng, YB Zhou, J Li…

Index: Luo, Yu; Liu, Hao-Min; Su, Ming-Bo; Sheng, Li; Zhou, Yu-Bo; Li, Jia; Lu, Wei Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 16 p. 4844 - 4846

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Citation Number: 10

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.