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
文献类型：期刊论文
| 作者 | Zou, Haixia1,2,3; Zhou, Liyan1; Li, Yuanzhen1; Cui, Yi1; Zhong, Hanbing1; Pan, Zhengying1; Yang, Zhen1,2,3; Quan, Junmin1 |
| 刊名 | JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2010-02-11 |
| 卷号 | 53期号:3页码:994-1003 |
| ISSN号 | 0022-2623 |
| DOI | 10.1021/jm9013373 |
| 英文摘要 | 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 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. |
| 语种 | 英语 |
| WOS记录号 | WOS:000274270900007 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://ir.iccas.ac.cn/handle/121111/68895]  |
| 专题 | 中国科学院化学研究所 |
| 通讯作者 | Yang, Zhen |
| 作者单位 | 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 |
| 推荐引用方式 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. |
入库方式： OAI收割
来源：化学研究所
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