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

…, L Wang, X Hou, H Fu, W Song, W Tang, H Fang

Index: Han, Leiqiang; Wang, Lei; Hou, Xuben; Fu, Huansheng; Song, Weiguo; Tang, Weiping; Fang, Hao Bioorganic and Medicinal Chemistry, 2014 , vol. 22, # 5 p. 1529 - 1538

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Citation Number: 10

Abstract

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 ...