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

Huansheng Fu; Leiqiang Han; Xuben Hou; Yanyan Dun; Lei Wang; Xiaowei Gong; Hao Fang

doi:10.1016/j.bmc.2015.07.008

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. Epub 2015 Jul 11.

Authors

Huansheng Fu¹, Leiqiang Han¹, Xuben Hou¹, Yanyan Dun¹, Lei Wang¹, Xiaowei Gong², Hao Fang³

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: haofangcn@sdu.edu.cn.

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Benzamides / chemical synthesis*
Benzamides / chemistry*
Histone Deacetylase Inhibitors / chemical synthesis*
Histone Deacetylase Inhibitors / chemistry
Humans
Molecular Structure
Saccharin / chemical synthesis*
Saccharin / chemistry*
Structure-Activity Relationship

Substances

Benzamides
Histone Deacetylase Inhibitors
Saccharin