Synthesis and Biological Evaluation of 3-Benzisoxazolyl-4-indolylmaleimides as Potent, Selective Inhibitors of Glycogen Synthase Kinase-3β

…, T Pang, L Xu, J Cao, L Han, Y Li, W Wang, J Gao, J Li

Index: Ye, Qing; Li, Meng; Zhou, Yubo; Pang, Tao; Xu, Lei; Cao, Jiayi; Han, Liang; Li, Yujin; Wang, Weisi; Gao, Jianrong; Li, Jia Molecules, 2013 , vol. 18, # 5 p. 5498 - 5516

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Citation Number: 6

Abstract

Abstract: A series of novel 3-benzisoxazolyl-4-indolyl-maleimides were synthesized and evaluated for their GSK-3β inhibitory activity. Most compounds exhibited high inhibitory potency towards GSK-3β. Among them, compound 7j with an IC 50 value of 0.73 nM was the most promising GSK-3β inhibitor. Preliminary structure-activity relationships were examined and showed that different substituents on the indole ring and N 1-position of the indole ...