Benzo [e] isoindole-1, 3-diones as potential inhibitors of glycogen synthase kinase-3 (GSK-3). Synthesis, kinase inhibitory activity, zebrafish phenotype, and modeling …

H Zou, L Zhou, Y Li, Y Cui, H Zhong, Z Pan…

Index: Zou, Haixia; Zhou, Liyan; Li, Yuanzhen; Cui, Yi; Zhong, Hanbing; Pan, Zhengying; Yang, Zhen; Quan, Junmin Journal of Medicinal Chemistry, 2010 , vol. 53, # 3 p. 994 - 1003

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Citation Number: 23

Abstract

Benzo [e] isoindole-1, 3-dione derivatives were synthesized, and the effects on GSK-3β activity and zebrafish embryo growth were evaluated. A series of derivatives show obvious inhibitory activity against GSK-3β. The most potent inhibitor, 7, 8-dimethoxy-5-methylbenzo [e] isoindole-1, 3-dione (8a), shows nanomolar IC50 and obvious phenotype on zebrafish embryo growth associated with the inhibition of GSK-3β at low micromolar concentration. ...

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