title: 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.
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.
authors: 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.
authors: Leiqiang
authors: L
authors: Han
authors: 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.
authors: Lei
authors: L
authors: Wang
authors: 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.
authors: Xuben
authors: X
authors: Hou
authors: 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.
authors: Huansheng
authors: H
authors: Fu
authors: 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.
authors: Weiguo
authors: W
authors: Song
authors: Division of Pharmaceutical Sciences, School of Pharmacy, University of Wisconsin, Madison 53705, USA.
authors: Weiping
authors: W
authors: Tang
authors: 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.
authors: Hao
authors: H
authors: Fang
mesh_terms: D049109:Cell Proliferation; D015195:Drug Design; D056572:Histone Deacetylase Inhibitors / Q000737:chemistry*; D006655:Histone Deacetylases / Q000737:chemistry* / Q000378:metabolism; D006877:Hydroxamic Acids / Q000138:chemical synthesis* / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: D056572:Histone Deacetylase Inhibitors; D006877:Hydroxamic Acids; D006655:Histone Deacetylases
keywords: 1,2-Dihydrobenzo[d]isothiazol-3-one-1,1-dioxide; Antiproliferative; Histone deacetylase inhibitor