Synthesis and Evaluation of Optical Properties, SHP2 Inhibitory Activity, and Cellular Imaging for Novel 2-Quinolone Derivatives
文献类型：期刊论文
| 作者 | Zhang, Chun1; Yang, Yuting1; Gao, Li-Xin1,3; Gan, Suya1; Li, Jia3 ; Wang, Xin2; Zhou, Yu-Bo3,4; Wang, Wen-Long1
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| 刊名 | ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
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| 出版日期 | 2025-03-17 |
| 页码 | 10 |
| 关键词 | Fluorescent inhibitors SHP2 2-quinolone derivatives optical properties drug tracing medical diagnosis |
| ISSN号 | 1871-5206 |
| DOI | 10.2174/0118715206337347250219112715 |
| 英文摘要 | Introduction Although the development of SHP2 inhibitors has made striking progress, there is no inhibitor in clinical evaluation because of the potential side effects induced by poor drug distribution. Fluorescence imaging technology is widely used in the process of diagnosis and treatment of diseases because of the advantages of rapid imaging and non-destructive detection and might provide a new way to explore the mechanism of drug-target interactions in intact tissue.Methods A series of 2-quinolone derivatives as fluorescent inhibitors against SHP2 were designed and synthesized, and their spectral properties and biological activities were evaluated in this report. The representative compound 8A had excellent fluorescence properties (lambda maxemi: 562 nm, Stokes shift: 170 nm, fluorescence quantum yield: 0.072) and optical stability.Results Moreover, compound 8A emitted a blue signal in SHP2WT U2OS cells and inhibited the SHP2 enzyme abilities (IC50: 20.16 +/- 0.95 mu M) without the extra combination of suitable fluorophores, linker, or selective-activated molecules.Conclusion Therefore, we hope that compound 8A could act as a lead to develop novel, convenient, and bifunctional chemical tools to explore the mechanism of drug-target interactions in intact tissue and promote the integrated research progress of diagnosis and treatment of SHP2 related diseases. |
| WOS关键词 | INDUCED FLUORESCENCE EMISSION ; TYROSINE ; IDENTIFICATION ; QUINOLINES ; VERSATILE |
| 资助项目 | National Natural Science Foundation of China[22277043] ; National Natural Science Foundation of China[21772068] ; Fundamental Research Funds for the Central Universities[JUSRP121065] ; High-Level Personnel Project of Jiangsu Province[JSSCBS20210848] |
| WOS研究方向 | Oncology ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:001459289300001 |
| 出版者 | BENTHAM SCIENCE PUBL LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/316905]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Wang, Xin; Zhou, Yu-Bo; Wang, Wen-Long |
| 作者单位 | 1.Jiangnan Univ, Sch Life Sci & Hlth Engn, Wuxi 214122, Jiangsu, Peoples R China 2.Henan Univ, Henan Macquarie Univ Joint Ctr Biomed Innovat, Sch Life Sci, Kaifeng 475004, Henan, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, State Key Lab Drug Res, Shanghai 201203, Peoples R China 4.Chinese Acad Sci, Zhongshan Inst Drug Discovery, Shanghai Inst Mat Med, SSIP Healthcare & Med Demonstrat Zone, Zhongshan 528400, Guangdong, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhang, Chun,Yang, Yuting,Gao, Li-Xin,et al. Synthesis and Evaluation of Optical Properties, SHP2 Inhibitory Activity, and Cellular Imaging for Novel 2-Quinolone Derivatives[J]. ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY,2025:10. |
| APA | Zhang, Chun.,Yang, Yuting.,Gao, Li-Xin.,Gan, Suya.,Li, Jia.,...&Wang, Wen-Long.(2025).Synthesis and Evaluation of Optical Properties, SHP2 Inhibitory Activity, and Cellular Imaging for Novel 2-Quinolone Derivatives.ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY,10. |
| MLA | Zhang, Chun,et al."Synthesis and Evaluation of Optical Properties, SHP2 Inhibitory Activity, and Cellular Imaging for Novel 2-Quinolone Derivatives".ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY (2025):10. |
入库方式： OAI收割
来源：上海药物研究所
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