Design, synthesis and evaluation of 7-azaindazolyl-indolyl-maleimides as glycogen synthase kinase-3β (GSK-3β) inhibitors

Q Ye, Y Shen, Y Zhou, D Lv, J Gao, J Li, Y Hu

文献索引：Ye, Qing; Shen, Yanhong; Zhou, Yubo; Lv, Dan; Gao, Jianrong; Li, Jia; Hu, Yongzhou European Journal of Medicinal Chemistry, 2013 , vol. 68, p. 361 - 371

全文：HTML全文

被引用次数: 7

摘要

Abstract A series of 7-azaindazolyl-indolyl-maleimides were designed, synthesized and evaluated for their GSK-3β inhibitory activity. Most compounds exhibited potent activity against GSK-3β. Among them, compounds 17a, 17b, 17g, 17i, 29a and 30 significantly reduced Aβ-induced Tau hyperphosphorylation, showin; g the inhibition of GSK-3β at the cell level. Preliminary structure–activity relationships were discussed based on the ...