Synthesis and biological evaluation of novel 4,5-bisindolyl-1,2,4-triazol-3-ones as glycogen synthase kinase-3 beta inhibitors and neuroprotective agents
文献类型：期刊论文
| 作者 | Hu, Yuanyuan; Ruan, Wenchen; Gao, Anhui; Zhou, Yubo ; Gao, Lixin; Xu, Meng; Gao, Jianrong; Ye, Qing; Li, Jia1; Pang, Tao2
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| 刊名 | PHARMAZIE
 |
| 出版日期 | 2017-12 |
| 卷号 | 72期号:12页码:707-713 |
| ISSN号 | 0031-7144 |
| DOI | 10.1691/ph.2017.7722 |
| 文献子类 | Article |
| 英文摘要 | A series of novel 4,5-bisindolyl-1,2,4-triazol-3-ones were designed, prepared and evaluated for their glycogen synthase kinase (GSK)-3 beta inhibitory activities. Compounds exhibited favorable inhibitory potency towards GSK-3 beta kinase at the molecular level and in cells indicated by significantly reducing GSK-3 beta substrate Tau phosphorylation at Ser396 in primary neurons showing the inhibition of cellular GSK-3 beta. In an in vitro model of neuronal injury, compounds 6b, 6d and 6f prevented glutamate-induced neuronal death which was closely associated with cerebral ischemic stroke. Preliminary structure-activity relationship was examined and showed that different substituents on the indole ring had significant influences on the GSK-3 beta inhibitory potency. These findings may provide new insights into the development of novel GSK-3 beta inhibitors as neuroprotective agents. |
| WOS关键词 | PROTEIN-KINASE-C ; VALPROIC ACID ; LITHIUM ; GLUTAMATE ; ISCHEMIA ; NEURONS ; POTENT ; ROLES ; GSK3 |
| 资助项目 | Natural Science Foundation of Zhejiang Province[LY14H300003] ; Postdoctoral Science Foundation of China[2014M550256] ; State Key Laboratory of Drug Research[SIMMM1601KF-04] ; National Natural Science Foundation of China[21402241] ; Natural Science Foundation of Jiangsu Province[BK20160032] ; Six Talent Peaks Project of Jiangsu Province[00000000] ; Program for Jiangsu Province "Shuang Chuang" Team[00000000] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000426406700001 |
| 出版者 | GOVI-VERLAG PHARMAZEUTISCHER VERLAG GMBH |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/272360]  |
| 专题 | 国家新药筛选中心 中科院受体结构与功能重点实验室 新药研究国家重点实验室 药物安全性评价中心 |
| 通讯作者 | Ye, Qing |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 2.China Pharmaceut Univ, Jiangsu Key Lab Drug Screening, Nanjing, Jiangsu, Peoples R China |
| 推荐引用方式 GB/T 7714 | Hu, Yuanyuan,Ruan, Wenchen,Gao, Anhui,et al. Synthesis and biological evaluation of novel 4,5-bisindolyl-1,2,4-triazol-3-ones as glycogen synthase kinase-3 beta inhibitors and neuroprotective agents[J]. PHARMAZIE,2017,72(12):707-713. |
| APA | Hu, Yuanyuan.,Ruan, Wenchen.,Gao, Anhui.,Zhou, Yubo.,Gao, Lixin.,...&Pang, Tao.(2017).Synthesis and biological evaluation of novel 4,5-bisindolyl-1,2,4-triazol-3-ones as glycogen synthase kinase-3 beta inhibitors and neuroprotective agents.PHARMAZIE,72(12),707-713. |
| MLA | Hu, Yuanyuan,et al."Synthesis and biological evaluation of novel 4,5-bisindolyl-1,2,4-triazol-3-ones as glycogen synthase kinase-3 beta inhibitors and neuroprotective agents".PHARMAZIE 72.12(2017):707-713. |
入库方式： OAI收割
来源：上海药物研究所
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