title: Design, synthesis and bioevalution of novel benzamides derivatives as HDAC inhibitors.
abstract: A series of novel benzamides derivatives was designed and synthesized as HDAC inhibitors. Exploration of the structure-activity relationships resulted in compounds that are potent in vitro. In addition, the best compound 1a exhibited an acceptable pharmacokinetic profile with bioavailability in rat of 81% and could be considered as a candidate compound for further development.
authors.affiliation: The General Hospital of Chinese People's Liberation Army, Beijing 100853, China.
authors.forename: Yanyang
authors.initials: Y
authors.lastname: Li
authors.forename: Yan
authors.initials: Y
authors.lastname: Zhou
authors.forename: Pengyu
authors.initials: P
authors.lastname: Qian
authors.forename: Yongzhen
authors.initials: Y
authors.lastname: Wang
authors.forename: Falong
authors.initials: F
authors.lastname: Jiang
authors.forename: Zhenglin
authors.initials: Z
authors.lastname: Yao
authors.forename: Wenxiang
authors.initials: W
authors.lastname: Hu
authors.forename: Yanjin
authors.initials: Y
authors.lastname: Zhao
authors.forename: Shuxin
authors.initials: S
authors.lastname: Li
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000633:toxicity; D001549:Benzamides / Q000138:chemical synthesis* / Q000737:chemistry* / Q000493:pharmacokinetics / Q000633:toxicity; D045744:Cell Line, Tumor; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D004354:Drug Screening Assays, Antitumor; D045325:HCT116 Cells; D006207:Half-Life; D056572:Histone Deacetylase Inhibitors / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000633:toxicity; D006655:Histone Deacetylases / Q000737:chemistry* / Q000378:metabolism; D006801:Humans; D061986:MCF-7 Cells; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000633:toxicity; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D001549:Benzamides; D056572:Histone Deacetylase Inhibitors; D011743:Pyrimidines; D006655:Histone Deacetylases