Design, synthesis and biological evaluation of benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of glycogen synthase kinase-3β (GSK-3β)

P Zhang, HR Hu, SH Bian, ZH Huang, Y Chu…

Index: Zhang, Peng; Hu, Hai-Rong; Bian, Shi-Hui; Huang, Zhao-Hui; Chu, Yong; Ye, De-Yong European Journal of Medicinal Chemistry, 2013 , vol. 61, p. 95 - 103

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Citation Number: 10

Abstract

Glycogen synthase kinase-3β (GSK-3β) plays a key role in type II diabetes and Alzheimer's diseases, to which non-ATP competitive inhibitors represent an effectively therapeutical approach due to their good specificity. Herein, a series of small molecules benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of GSK-3β have been designed and synthesized. The in vitro evaluation performed by luminescent assay ...