Synthesis and structure-activity relationship study of pyrazolo[3,4-d]pyrimidines as tyrosine kinase RET inhibitors
文献类型：期刊论文
| 作者 | Wang, Chengyan1; Liu, Hongchun3 ; Song, Zilan2; Ji, Yinchun3; Xing, Li2; Peng, Xia3; Wang, Xisheng1; Ai, Jing3; Geng, Meiyu3; Zhang, Ao2
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
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| 出版日期 | 2017-06-01 |
| 卷号 | 27期号:11页码:2544-2548 |
| 关键词 | Tyrosine kinase RET Pyrazolo[3,4-d]pyrimidine Anticancer Cell proliferation Structure-activity relationship |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2017.03.088 |
| 文献子类 | Article |
| 英文摘要 | Three series of pyrazolo[3,4-d]pyrimidine derivatives were synthesized and evaluated as RET kinase inhibitors. Compounds 23a and 23c were identified to show significant activity both in the biochemical and the BaF3/CCDC6-RET cell assays. Compound 23c was found to significantly inhibit RET phosphorylation and down-stream signaling in BaF3/CCDC6-RET cells, confirming its potent cellular RET-targeting profile. Different from other RET inhibitors with equal potency against KDR that associated with severe toxicity, 23c did not show significant KDR-inhibition even at the concentration of 1 mu M. These results demonstrated that 23c is a potent and selective RET inhibitor. (C) 2017 Elsevier Ltd. All rights reserved. |
| WOS关键词 | MEDULLARY-THYROID CANCER ; POTENT INHIBITOR ; CABOZANTINIB ; DERIVATIVES ; ONCOGENE |
| 资助项目 | Chinese NSF[81430080] ; Chinese NSF[81373277] ; Chinese NSF[81473243] ; National Program on Key Basic Research Project of China[2015CB910603] ; Key Program of the Frontier Science of the Chinese Academy of Sciences[160621] ; [GJHZ1622] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000402023800053 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/272649]  |
| 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 | Wang, Xisheng; Ai, Jing; Zhang, Ao |
| 作者单位 | 1.Univ Sci & Technol China, Nano Sci & Technol Inst, Suzhou 215123, Peoples R China; 2.Chinese Acad Sci, SIMM, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China; 3.Chinese Acad Sci, SIMM, Div Antitumor Pharmacol, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang, Chengyan,Liu, Hongchun,Song, Zilan,et al. Synthesis and structure-activity relationship study of pyrazolo[3,4-d]pyrimidines as tyrosine kinase RET inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2017,27(11):2544-2548. |
| APA | Wang, Chengyan.,Liu, Hongchun.,Song, Zilan.,Ji, Yinchun.,Xing, Li.,...&Zhang, Ao.(2017).Synthesis and structure-activity relationship study of pyrazolo[3,4-d]pyrimidines as tyrosine kinase RET inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,27(11),2544-2548. |
| MLA | Wang, Chengyan,et al."Synthesis and structure-activity relationship study of pyrazolo[3,4-d]pyrimidines as tyrosine kinase RET inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 27.11(2017):2544-2548. |
入库方式： OAI收割
来源：上海药物研究所
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