Synthesis and biological evaluation of piperamide analogues as HDAC inhibitors

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 fe...

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Published inBioorganic & medicinal chemistry letters Vol. 21; no. 16; pp. 4844 - 4846
Main Authors Luo, Yu, Liu, Hao-Min, Su, Ming-Bo, Sheng, Li, Zhou, Yu-Bo, Li, Jia, Lu, Wei
Format Journal Article
LanguageEnglish
Published Amsterdam Elsevier Ltd 15.08.2011
Elsevier
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Summary: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.
Bibliography:ObjectType-Article-2
SourceType-Scholarly Journals-1
ObjectType-Feature-1
content type line 23
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2011.06.046