Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors
文献类型：期刊论文
| 作者 | Zhao, Bin2; Li, Yixuan3; Xu, Pan1; Dai, Yang3; Luo, Cheng1 ; Sun, Yiming3; Ai, Jing3; Geng, Meiyu3; Duan, Wenhu2
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| 刊名 | ACS MEDICINAL CHEMISTRY LETTERS
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| 出版日期 | 2016-06 |
| 卷号 | 7期号:6页码:629-634 |
| 关键词 | Cancer FGFR inhibitor pyrazolo[3,4-b]pyridine |
| ISSN号 | 1948-5875 |
| DOI | 10.1021/acsmedchemlett.6b00066 |
| 文献子类 | Article |
| 英文摘要 | Fibroblast growth factor receptors (FGFRs) are important targets for cancer therapy. Herein, we describe the design, synthesis, and biological evaluation of a novel series of 1H-pyrazolo[3,4-b]pyridine derivatives as potent and selective FGFR kinase inhibitors. On the basis of its excellent in vitro potency and favorable pharmacokinetic properties, compound 7n was selected for in vivo evaluation and showed significant antitumor activity in a FGFR1-driven H1581 xenograft model. These results indicated that 7n would be a promising candidate for further drug development. |
| WOS关键词 | RECEPTOR TYROSINE KINASE ; CANCER ; ANGIOGENESIS ; MANAGEMENT ; FAMILY |
| 资助项目 | National Natural Science Foundation of China[81273365] ; National Natural Science Foundation of China[81573271] ; National Natural Science Foundation of China[81473243] ; National Natural Science Foundation of China[81321092] ; National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program"[2014ZX09304002-008-001] ; Shanghai Science and Technology Commission[1315431901300] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000377845200018 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276019]  |
| 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 | Ai, Jing; Geng, Meiyu; Duan, Wenhu |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Drug Discovery & Design Ctr, State Key Lab Drug Res, 555 Zu Chong Zhi Rd, Shanghai 201203, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 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 | Zhao, Bin,Li, Yixuan,Xu, Pan,et al. Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors[J]. ACS MEDICINAL CHEMISTRY LETTERS,2016,7(6):629-634. |
| APA | Zhao, Bin.,Li, Yixuan.,Xu, Pan.,Dai, Yang.,Luo, Cheng.,...&Duan, Wenhu.(2016).Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors.ACS MEDICINAL CHEMISTRY LETTERS,7(6),629-634. |
| MLA | Zhao, Bin,et al."Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors".ACS MEDICINAL CHEMISTRY LETTERS 7.6(2016):629-634. |
入库方式： OAI收割
来源：上海药物研究所
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