2. Academic Validation
  3. Design, synthesis and preliminary bioactivity studies of 1,2-dihydrobenzo[d]isothiazol-3-one-1,1-dioxide hydroxamic acid derivatives as novel histone deacetylase inhibitors

Design, synthesis and preliminary bioactivity studies of 1,2-dihydrobenzo[d]isothiazol-3-one-1,1-dioxide hydroxamic acid derivatives as novel histone deacetylase inhibitors

  • Bioorg Med Chem. 2014 Mar 1;22(5):1529-38. doi: 10.1016/j.bmc.2014.01.045.
Leiqiang Han 1,  Lei Wang 1,  Xuben Hou 1,  Huansheng Fu 1,  Weiguo Song 1,  Weiping Tang 2,  Hao Fang 3
Affiliations

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, PR China.
  • 2 Division of Pharmaceutical Sciences, School of Pharmacy, University of Wisconsin, Madison 53705, USA.
  • 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, PR China. Electronic address: haofangcn@sdu.edu.cn.
PMID: 24525003 DOI: 10.1016/j.bmc.2014.01.045
Abstract

Histone deacetylase (HDAC) is a clinically validated target for antitumor therapy. In order to increase HDAC inhibition and efficiency, we developed a novel series of saccharin hydroxamic acids as potent HDAC inhibitors. Among them, compounds 11e, 11m, 11p exhibited similar or better HDACs inhibitory activity compared with the approved drug SAHA. Further biological evaluation indicated that compound 11m had potent antiproliferative activities against MDA-MB-231 and PC-3.

Keywords

1,2-Dihydrobenzo[d]isothiazol-3-one-1,1-dioxide; Antiproliferative; Histone deacetylase inhibitor.

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