ICCAS OpenIR
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
Zou, Haixia1,2,3; Zhou, Liyan1; Li, Yuanzhen1; Cui, Yi1; Zhong, Hanbing1; Pan, Zhengying1; Yang, Zhen1,2,3; Quan, Junmin1
2010-02-11
Source PublicationJOURNAL OF MEDICINAL CHEMISTRY
ISSN0022-2623
Volume53Issue:3Pages:994-1003
AbstractBenzo[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 IC(50) 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.
DOI10.1021/jm9013373
Indexed BySCI ; IC
Language英语
WOS IDWOS:000274270900007
PublisherAMER CHEMICAL SOC
Citation statistics
Cited Times:30[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://ir.iccas.ac.cn/handle/121111/68896
Collection中国科学院化学研究所
Corresponding AuthorYang, Zhen
Affiliation1.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
Recommended Citation
GB/T 7714
Zou, Haixia,Zhou, Liyan,Li, Yuanzhen,et al. 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[J]. JOURNAL OF MEDICINAL CHEMISTRY,2010,53(3):994-1003.
APA Zou, Haixia.,Zhou, Liyan.,Li, Yuanzhen.,Cui, Yi.,Zhong, Hanbing.,...&Quan, Junmin.(2010).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.JOURNAL OF MEDICINAL CHEMISTRY,53(3),994-1003.
MLA Zou, Haixia,et al."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".JOURNAL OF MEDICINAL CHEMISTRY 53.3(2010):994-1003.
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