Discovery and Biological Evaluation of a Series of Pyrrolo[2,3-b]pyrazines as Novel FGFR Inhibitors
文献类型：期刊论文
| 作者 | Zhang, Yan2,3; Liu, Hongchun3 ; Zhang, Zhen1,4; Wang, Ruifeng1,4; Liu, Tongchao1,4; Wang, Chaoyun2; Ma, Yuchi1; Ai, Jing3; Zhao, Dongmei4; Shen, Jingkang1
|
| 刊名 | MOLECULES
 |
| 出版日期 | 2017-04 |
| 卷号 | 22期号:4 |
| ISSN号 | 1420-3049 |
| 关键词 | FGFR1 inhibitor kinase inhibitor pyrazine hinge binder |
| DOI | 10.3390/molecules22040583 |
| 文献子类 | Article |
| 英文摘要 | Abnormality of fibroblast growth factor receptor (FGFR)-mediated signaling pathways were frequently found in various human malignancies, making FGFRs hot targets for cancer treatment. To address the consistent need for a new chemotype of FGFR inhibitors, here, we started with a hit structure identified from our internal hepatocyte growth factor receptor (also called c-Met) inhibitor project, and conducted a chemical optimization. After exploring three parts of the hit compound, we finally discovered a new series of pyrrolo[2,3-b]pyrazine FGFR inhibitors, which contain a novel scaffold and unique molecular shape. We believe that our findings can help others to further develop selective FGFR inhibitors. |
| WOS关键词 | FACTOR RECEPTOR INHIBITORS ; FIBROBLAST ; KINASES ; DESIGN ; POTENT ; CANCERS ; FAMILY |
| 资助项目 | National Natural Science Foundation of China[81473243] ; NSFC-Shandong Joint Fund for Marine Science Research Centers[U1406402] ; Youth Innovation Promotion Association[00000000] ; "Personalized Medicines-Molecular Signature-based Drug Discovery and Development", Strategic Priority Research Program of the Chinese Academy of Sciences[XDA12020317] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Chemistry |
| 语种 | 英语 |
| 出版者 | MDPI AG |
| WOS记录号 | WOS:000404517800081 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/272710]  |
| 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 药物化学研究室 |
| 通讯作者 | Ma, Yuchi; Ai, Jing; Xiong, Bing |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Dept Med Chem, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China; 2.Binzhou Med Univ, Sch Pharmaceut Sci, Yantai 264003, Shandong, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Div Antitumor Pharmacol, 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 |
| 推荐引用方式 GB/T 7714 | Zhang, Yan,Liu, Hongchun,Zhang, Zhen,et al. Discovery and Biological Evaluation of a Series of Pyrrolo[2,3-b]pyrazines as Novel FGFR Inhibitors[J]. MOLECULES,2017,22(4). |
| APA | Zhang, Yan.,Liu, Hongchun.,Zhang, Zhen.,Wang, Ruifeng.,Liu, Tongchao.,...&Xiong, Bing.(2017).Discovery and Biological Evaluation of a Series of Pyrrolo[2,3-b]pyrazines as Novel FGFR Inhibitors.MOLECULES,22(4). |
| MLA | Zhang, Yan,et al."Discovery and Biological Evaluation of a Series of Pyrrolo[2,3-b]pyrazines as Novel FGFR Inhibitors".MOLECULES 22.4(2017). |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。