Structure-Based Discovery of a Series of 5H-Pyrrolo[2,3-b]pyrazine FGFR Kinase Inhibitors
文献类型：期刊论文
| 作者 | Jiang, Alan1,2; Liu, Qiufeng3; Wang, Ruifeng4,5; Wei, Peng4,5; Dai, Yang2; Wang, Xin5 ; Xu, Yechun3; Ma, Yuchi5; Ai, Jing2; Shen, Jingkang5
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| 刊名 | MOLECULES
 |
| 出版日期 | 2018-03 |
| 卷号 | 23期号:3 |
| 关键词 | cancer FGFR kinase inhibitor pyrrolo[2,3-b]pyrazine |
| ISSN号 | 1420-3049 |
| DOI | 10.3390/molecules23030698 |
| 文献子类 | Article |
| 英文摘要 | Fibroblast growth factor receptors (FGFRs), a subfamily of receptor tyrosine kinases, are aberrant in various cancer types, and considered to be promising targets for cancer therapy. We started with a weak-active compound that was identified from our internal hepatocyte growth factor receptor (also called c-Met) inhibitor project, and optimized it with the guidance of a co-crystal structure of compound 8 with FGFR1. Through rational design, synthesis, and the biological evaluation of a series of 5H-pyrrolo[2,3-b]pyrazine derivatives, we discovered several potent FGFR kinase inhibitors. Among them, compound 13 displayed high selectivity and favorable metabolic properties, demonstrating a promising lead for further development. |
| WOS关键词 | GROWTH-FACTOR RECEPTORS ; CH5183284/DEBIO 1347 ; SELECTIVE INHIBITOR ; TARGETING FGFR ; CANCER ; POTENT ; FAMILY ; AZD4547 ; MODELS ; LUNG |
| 资助项目 | National Natural Science Foundation of China[81661148046] ; National Natural Science Foundation of China[81773762] ; Personalized Medicines Molecular Signature-based Drug Discovery and Development[00000000] ; Strategic Priority Research Program of the Chinese Academy of Sciences[XDA12020317] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000428514100189 |
| 出版者 | MDPI |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279862]  |
| 专题 | 药理学第一研究室 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 药物发现与设计中心 药物化学研究室 |
| 通讯作者 | Xu, Yechun; Ma, Yuchi; Ai, Jing; Xiong, Bing |
| 作者单位 | 1.Nanchang Univ, Coll Pharm, 461 Bayi Ave, Nanchang 330006, Jiangxi, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Div Antitumor Pharmacol, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, Drug Design & Discovery Ctr, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China; 4.Shenyang Pharmaceut Univ, Minist Educ, Key Lab Struct Based Drug Design & Discovery, Shenyang 110016, Peoples R China; 5.Chinese Acad Sci, Shanghai Inst Mat Med, Dept Med Chem, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Jiang, Alan,Liu, Qiufeng,Wang, Ruifeng,et al. Structure-Based Discovery of a Series of 5H-Pyrrolo[2,3-b]pyrazine FGFR Kinase Inhibitors[J]. MOLECULES,2018,23(3). |
| APA | Jiang, Alan.,Liu, Qiufeng.,Wang, Ruifeng.,Wei, Peng.,Dai, Yang.,...&Xiong, Bing.(2018).Structure-Based Discovery of a Series of 5H-Pyrrolo[2,3-b]pyrazine FGFR Kinase Inhibitors.MOLECULES,23(3). |
| MLA | Jiang, Alan,et al."Structure-Based Discovery of a Series of 5H-Pyrrolo[2,3-b]pyrazine FGFR Kinase Inhibitors".MOLECULES 23.3(2018). |
入库方式： OAI收割
来源：上海药物研究所
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