Design, synthesis and biological evaluation of saccharin-based N-hydroxybenzamides as histone deacetylases (HDACs) inhibitors

  • Bioorg Med Chem. 2015 Sep 1;23(17):5774-81. doi: 10.1016/j.bmc.2015.07.008.
Huansheng Fu  1 ,  Leiqiang Han  1 ,  Xuben Hou  1 ,  Yanyan Dun  1 ,  Lei Wang  1 ,  Xiaowei Gong  2 ,  Hao Fang  3
Affiliations
  • 1. Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmacy, Shandong University, 44 West Wenhua Rd, Ji'nan 250012, China.
  • 2. Shandong Provincial Key Laboratory of Neuroprotective Drug, Shandong Qidu Pharmaceutical Co., Ltd, 250012, China.
  • 3. Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmacy, Shandong University, 44 West Wenhua Rd, Ji'nan 250012, China. Electronic address: [email protected].
PMID: 26216016 DOI: 10.1016/j.bmc.2015.07.008
Abstract

We report the development of a novel series of saccharin-based N-hydroxybenzamides as histone deacetylases inhibitors. Among them, 6 j exhibited potent HDACs inhibitory activity against Hela nuclear extract. Further biological evaluation found 6 i showed similar antiproliferative activities in vitro compared with the approved SAHA.

Keywords
Histone deacetylases inhibitor; N-Hydroxybenzamide; Saccharin.