title: Synthesis and biological evaluation of piperamide analogues as HDAC inhibitors.
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.
authors: Department of Chemistry, East China Normal University, 3663 North Zhongshan Road, Shanghai 200062, PR China.
authors: Yu
authors: Y
authors: Luo
authors: Hao-Min
authors: HM
authors: Liu
authors: Ming-Bo
authors: MB
authors: Su
authors: Li
authors: L
authors: Sheng
authors: Yu-Bo
authors: YB
authors: Zhou
authors: Jia
authors: J
authors: Li
authors: Wei
authors: W
authors: Lu
mesh_terms: D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D052117:Benzodioxoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004148:Dioxolanes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D056572:Histone Deacetylase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006655:Histone Deacetylases / Q000378:metabolism*; D006801:Humans; D015394:Molecular Structure; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D010881:Piperidones
chemical_list: D000577:Amides; D052117:Benzodioxoles; D004148:Dioxolanes; D056572:Histone Deacetylase Inhibitors; D006655:Histone Deacetylases; D011994:Recombinant Proteins; C568084:refrofractamide A; C498077:piperlongumine; D010881:Piperidones