Perfluoro-tert-butyl Group-Derived Capmatinib: Synthesis, Biological Evaluation and Its Application in F-19 Magnetic Resonance Imaging
文献类型：期刊论文
| 作者 | Zhang, Xinnan1; Wang, Luting2; Huang, Ruimin2 ; Wang, Jingbo3; Yan, Qifan1
|
| 刊名 | CHEMBIOCHEM
 |
| 出版日期 | 2023-08-16 |
| 页码 | 9 |
| 关键词 | F-19 MRI Capmatinib derivatives Targeted imaging Fluorinated derivatization Bioimaging |
| ISSN号 | 1439-4227 |
| DOI | 10.1002/cbic.202300354 |
| 通讯作者 | Huang, Ruimin(rmhuang@simm.ac.cn) ; Wang, Jingbo(wangjingbo1425@vip.163.com) ; Yan, Qifan(yanqifan@ecust.edu.cn) |
| 英文摘要 | Capmatinib is an FDA-approved drug to treat metastatic non-small cell lung cancer with MET-exon 14 skipping. Herein, the perfluoro-tert-butyl group, which possesses nine chemically identical fluorine atoms, was introduced on Capmatinib to afford a targeted F-19 magnetic resonance imaging (MRI) probe, perfluoro-tert-butyl group-derived Capmatinib (9F-CAP). The F-19 MRI concentration limit was found to be 25 mM in FLASH sequence. Molecular docking simulation, surface plasmon resonance (SPR) (with a K-d of 40.7 & mu;M), half-inhibitory concentration (with a IC50 of 168 nM), Annexin V, and cytotoxicity assays jointly demonstrated that the 9F-CAP targeted cMET protein specifically. Therefore, the targeted imaging capability of 9F-CAP is of great significance for the preoperative diagnosis of specific cancers. |
| WOS关键词 | MRI AGENTS ; PROBE ; DESIGN ; CANCER |
| 资助项目 | Fundamental Research Funds for the Central Universities[222201717003] ; National Natural Science Foundation of China[82172001] ; Fundamental research program funding of Ninth People's Hospital affiliated to Shanghai Jiao Tong university School of Medicine[JYZZ185] ; Class B project of the fifth Nova Program of Shanghai Institute of Materia Medica, Chinese Academy of Sciences |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:001049324100001 |
| 出版者 | WILEY-V C H VERLAG GMBH |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/306935]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Huang, Ruimin; Wang, Jingbo; Yan, Qifan |
| 作者单位 | 1.East China Univ Sci & Technol, Prize Scientist Joint Res Ctr, Sch Chem & Mol Engn, Key Lab Adv Mat & Feringa Nobel, 130 Meilong Rd, Shanghai 200237, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China 3.Shanghai Jiao Tong Univ, Shanghai Peoples Hosp 9, Sch Med, 639 Zhizaoju Rd, Shanghai 200025, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhang, Xinnan,Wang, Luting,Huang, Ruimin,et al. Perfluoro-tert-butyl Group-Derived Capmatinib: Synthesis, Biological Evaluation and Its Application in F-19 Magnetic Resonance Imaging[J]. CHEMBIOCHEM,2023:9. |
| APA | Zhang, Xinnan,Wang, Luting,Huang, Ruimin,Wang, Jingbo,&Yan, Qifan.(2023).Perfluoro-tert-butyl Group-Derived Capmatinib: Synthesis, Biological Evaluation and Its Application in F-19 Magnetic Resonance Imaging.CHEMBIOCHEM,9. |
| MLA | Zhang, Xinnan,et al."Perfluoro-tert-butyl Group-Derived Capmatinib: Synthesis, Biological Evaluation and Its Application in F-19 Magnetic Resonance Imaging".CHEMBIOCHEM (2023):9. |
入库方式： OAI收割
来源：上海药物研究所
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