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  • Title: Design, synthesis and evaluation of 7-azaindazolyl-indolyl-maleimides as glycogen synthase kinase-3β (GSK-3β) inhibitors.
    Author: Ye Q, Shen Y, Zhou Y, Lv D, Gao J, Li J, Hu Y.
    Journal: Eur J Med Chem; 2013 Oct; 68():361-71. PubMed ID: 23994329.
    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 experimental data obtained.
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