Design, synthesis and bioevalution of novel benzamides derivatives as HDAC inhibitors

A series of novel benzamides derivatives was designed and synthesized as HDAC inhibitors. 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 bes...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2013-01, Vol.23 (1), p.179-182
Hauptverfasser:	Li, Yanyang, Zhou, Yan, Qian, Pengyu, Wang, Yongzhen, Jiang, Falong, Yao, Zhenglin, Hu, Wenxiang, Zhao, Yanjin, Li, Shuxin
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antineoplastic Agents - chemical synthesis Antineoplastic Agents - pharmacokinetics Antineoplastic Agents - toxicity Antiproliferative activity Benzamide derivatives benzamides Benzamides - chemical synthesis Benzamides - chemistry Benzamides - pharmacokinetics Benzamides - toxicity Bioavailability Cell Line, Tumor Drug Design Drug Evaluation, Preclinical Drug Screening Assays, Antitumor Half-Life HCT116 Cells HDAC Histone Deacetylase Inhibitors - chemical synthesis Histone Deacetylase Inhibitors - pharmacokinetics Histone Deacetylase Inhibitors - toxicity Histone Deacetylases - chemistry Histone Deacetylases - metabolism Humans MCF-7 Cells pharmacokinetics Pyrimidines - chemical synthesis Pyrimidines - pharmacokinetics Pyrimidines - toxicity Rats Structure-Activity Relationship structure-activity relationships
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Zusammenfassung:	A series of novel benzamides derivatives was designed and synthesized as HDAC inhibitors. 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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2012.10.114