Maksym O. Chekanov, O. V. Ostrynska, Anatoliy R Synyugin
May 15, 2014
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Influential Citations
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Journal
Journal of Enzyme Inhibition and Medicinal Chemistry
Abstract
Abstract The synthesis and in vitro evaluation of 40 new 2-phenylisothiazolidin-3-one-1,1-dioxide derivatives are described. The optimization based on biological screening data and molecular modeling resulted in a 10-fold increase in inhibitory activity compared with previously reported inhibitors of this class and led to the identification of 3-{[2-chloro-4-(1,1-dioxido-3-oxoisothiazolidin-2-yl)benzoyl]amino}benzoic acid, a potent inhibitor of human protein kinase CK2 (ІC50 = 1.5 μM).