Synthesis of triazolotriazine derivatives as c-Met inhibitors
文献类型：期刊论文
| 作者 | Guo, Yuting1,2; Peng, Xia3; Ji, Yinchun3; Zhang, Yitong1,3; Ding, Jian1,3 ; Zhan, Zhengsheng2; Ai, Jing1,3; Duan, Wenhu1,2
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| 刊名 | MOLECULAR DIVERSITY
 |
| 出版日期 | 2020-03-10 |
| 页码 | 8 |
| 关键词 | Receptor tyrosine kinase c-Met Triazolotriazine SAR Cellular potency |
| ISSN号 | 1381-1991 |
| DOI | 10.1007/s11030-020-10067-5 |
| 通讯作者 | Zhan, Zhengsheng(zszhan@simm.ac.cn) ; Ai, Jing(jai@simm.ac.cn) ; Duan, Wenhu(whduan@simm.ac.cn) |
| 英文摘要 | Receptor tyrosine kinase c-Met is an important antitumor drug target. Triazolotriazine analogues2-10were prepared efficiently and evaluated the enzymatic and cellular c-Met activities. Brief structure-activity relationships of triazolotriazine core and CF2-quinoline part were investigated, leading to the discovery of compound8with nanomolar enzymatic c-Met activity, and subnanomolar MKN45 and EBC-1 cellular potencies. The proposed binding model of 8 and c-Met unraveled that two canonical hydrogen bonds and a pi-pi stacking interaction formed between the inhibitor and the ATP binding site of c-Met kinase domain, which accounted for its potent c-Met activities. [GRAPHICS] . |
| WOS关键词 | GROWTH-FACTOR RECEPTOR ; KINASE INHIBITOR ; HIGHLY POTENT ; DISCOVERY ; IDENTIFICATION ; PROTOONCOGENE ; CABOZANTINIB ; METASTASIS ; VOLITINIB ; PATHWAY |
| 资助项目 | Shanghai Sailing Program[17YF1423300] ; Youth Innovation Promotion Association of CAS[2018324] ; National Science and Technology Major Project Key New Drug Creation and Manufacturing Program, China[2018ZX09711002-011-016] ; Strategic Priority Research Program of the Chinese Academy of Sciences[XDA12020228] ; National Natural Science Foundation of China[21702220] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000562581300001 |
| 出版者 | SPRINGER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/292411]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Zhan, Zhengsheng; Ai, Jing; Duan, Wenhu |
| 作者单位 | 1.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, Dept Med Chem, 555 Zu Chong Zhi Rd, Shanghai 201203, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, Div Antitumor Pharmacol, State Key Lab Drug Res, 555 Zu Chong Zhi Rd, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Guo, Yuting,Peng, Xia,Ji, Yinchun,et al. Synthesis of triazolotriazine derivatives as c-Met inhibitors[J]. MOLECULAR DIVERSITY,2020:8. |
| APA | Guo, Yuting.,Peng, Xia.,Ji, Yinchun.,Zhang, Yitong.,Ding, Jian.,...&Duan, Wenhu.(2020).Synthesis of triazolotriazine derivatives as c-Met inhibitors.MOLECULAR DIVERSITY,8. |
| MLA | Guo, Yuting,et al."Synthesis of triazolotriazine derivatives as c-Met inhibitors".MOLECULAR DIVERSITY (2020):8. |
入库方式： OAI收割
来源：上海药物研究所
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