2. Academic Validation
  3. Design, synthesis and bioevalution of novel benzamides derivatives as HDAC inhibitors

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

  • Bioorg Med Chem Lett. 2013 Jan 1;23(1):179-82. doi: 10.1016/j.bmcl.2012.10.114.
Yanyang Li 1,  Yan Zhou,  Pengyu Qian,  Yongzhen Wang,  Falong Jiang,  Zhenglin Yao,  Wenxiang Hu,  Yanjin Zhao,  Shuxin Li
Affiliations

Affiliation

  • 1 The General Hospital of Chinese People's Liberation Army, Beijing 100853, China.
PMID: 23206867 DOI: 10.1016/j.bmcl.2012.10.114
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.

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