Benzo[e]isoindole-1,3-diones as Potential Inhibitors of Glycogen Synthase Kinase-3 (GSK-3). Synthesis, Kinase Inhibitory Activity, Zebrafish Phenotype, and Modeling of Binding Mode

被引：46
|
作者：
Zou, Haixia [1 ,2 ,3 ]
Zhou, Liyan [1 ]
Li, Yuanzhen [1 ]
Cui, Yi [1 ]
Zhong, Hanbing [1 ]
Pan, Zhengying [1 ]
Yang, Zhen [1 ,2 ,3 ]
Quan, Junmin [1 ]
机构：
[1] Peking Univ, Shenzhen Grad Sch, Lab Chem Genom, Shenzhen, Peoples R China
[2] Peking Univ, Coll Chem, BNLMS, Beijing 100871, Peoples R China
[3] Peking Univ, Minist Educ, Key Lab Bioorgan Chem & Mol Engn, Beijing 100871, Peoples R China
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 53卷 / 03期
基金：
美国国家科学基金会;
关键词：
SELECTIVE INHIBITORS; GSK-3; TARGET; ROLES;
D O I：
10.1021/jm9013373
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Benzo[e]isoindole-1,3-dione derivatives were synthesized, and the effects on GSK-3 beta activity and zebrafish embryo growth were evaluated. A series of derivatives show obvious inhibitory activity against GSK-3 beta. 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-3 beta at low micromolar concentration. The interaction mode between 8a and GSK-3 beta was characterized by computational modeling.
引用
收藏
页码：994 / 1003
页数：10
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