title: Design, synthesis and evaluation of 7-azaindazolyl-indolyl-maleimides as glycogen synthase kinase-3β (GSK-3β) inhibitors.
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.
authors.affiliation: ZJU-ENS Joint Laboratory of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China; State Key Laboratory Breeding Base of Green Chemistry-Synthesis Technology, Zhejiang University of Technology, Hangzhou 310032, China.
authors.forename: Qing
authors.initials: Q
authors.lastname: Ye
authors.forename: Yanhong
authors.initials: Y
authors.lastname: Shen
authors.forename: Yubo
authors.initials: Y
authors.lastname: Zhou
authors.forename: Dan
authors.initials: D
authors.lastname: Lv
authors.forename: Jianrong
authors.initials: J
authors.lastname: Gao
authors.forename: Jia
authors.initials: J
authors.lastname: Li
authors.forename: Yongzhou
authors.initials: Y
authors.lastname: Hu
mesh_terms: D001372:Aza Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D015153:Blotting, Western; D045744:Cell Line, Tumor; D015195:Drug Design; D004789:Enzyme Activation / Q000187:drug effects; D038362:Glycogen Synthase Kinase 3 / Q000037:antagonists & inhibitors*; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D008301:Maleimides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D015394:Molecular Structure; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D001372:Aza Compounds; D007211:Indoles; D008301:Maleimides; D047428:Protein Kinase Inhibitors; D038362:Glycogen Synthase Kinase 3
keywords: 7-Azaindazolyl-indolyl-maleimides; Cellular activity; Enzymatic activity; GSK-3β inhibitors