Novel imidazo[1,2,4] triazole derivatives: Synthesis, fluorescence, bioactivity for SHP1
文献类型：期刊论文
| 作者 | Yan, Xue3,4; Zhang, Chun3; Gao, Li-Xin2,3; Liu, Min -Min3; Yang, Yu-Ting3; Yu, Li-Jie3; Zhou, Yu-Bo2 ; Milaneh, Slieman1,3; Zhu, Yun-Long5; Li, Jia2
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| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
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| 出版日期 | 2024-02-05 |
| 卷号 | 265页码:15 |
| ISSN号 | 0223-5234 |
| 关键词 | Imidazo[124] triazole derivatives Fluorescence property SHP1 Bioactivity Cellular imaging |
| DOI | 10.1016/j.ejmech.2023.116027 |
| 通讯作者 | Zhu, Yun-Long(sequoia113847@163.com) ; Li, Jia(jli@simm.ac.cn) ; Wang, Wen-Long(wenlongwang@jiangnan.edu.cn) |
| 英文摘要 | The Src homology 2 domain-containing protein tyrosine phosphatase 1 (SHP1) is a convergent node for oncogenic cell-signaling cascades. Consequently, SHP1 represents a potential target for drug development in cancer treatment. The development of efficient methods for rapidly tracing and modulating the SHP1 activity in complex biological systems is of considerable significance for advancing the integration of diagnosis and treatment of the related disease. Thus, we designed and synthesized a series of imidazo[1,2,4] triazole derivatives containing salicylic acid to explore novel scaffolds with inhibitory activities and good fluorescence properties for SHP1. The photophysical properties and inhibitory activities of these imidazo[1,2,4] triazole derivatives (5a-5y) against SHP1PTP were thoroughly studied from the theoretical simulation and experimental application aspects. The representative compound 5p exhibited remarkable fluorescence response (P: 0.002) with fluorescence quantum yield (QY) of 0.37 and inhibitory rate of 85.21 +/- 5.17% against SHP1PTP at the concentration of 100 mu M. Furthermore, compound 5p showed obvious aggregation caused quenching (ACQ) effect and had high selectivity for Fe3+ ions, good anti-interference and relatively low detection limit (5.55 mu M). Finally, the cellular imaging test of compound 5p also exhibited good biocompatibility and certain potential biological imaging application. This study provides a potential way to develop molecules with fluorescent properties and bioactivities for SHP1. |
| WOS关键词 | PROTEIN-TYROSINE PHOSPHATASES ; DENSITY-FUNCTIONAL THEORY ; SMALL-MOLECULE INHIBITOR ; SALICYLIC-ACID ; SCHIFF-BASE ; HETEROCYCLES ; POTENT ; DISCOVERY ; ENZYMES ; PROBES |
| 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 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| WOS记录号 | WOS:001147238500001 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/308951]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Zhu, Yun-Long; Li, Jia; Wang, Wen-Long |
| 作者单位 | 1.Higher Inst Appl Sci & Technol, Dept Pharmaceut & Chem Ind, Damascus 31983, Syria 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China 3.Jiangnan Univ, Sch Life Sci & Hlth Engn, Wuxi 214122, Jiangsu, Peoples R China 4.Jiangnan Univ, Sch Chem & Mat Engn, Wuxi 214122, Jiangsu, Peoples R China 5.Jiangnan Univ, Wuxi Maternal & Child Hlth Hosp, Wuxi Sch Med, Wuxi 214002, Jiangsu, Peoples R China |
| 推荐引用方式 GB/T 7714 | Yan, Xue,Zhang, Chun,Gao, Li-Xin,et al. Novel imidazo[1,2,4] triazole derivatives: Synthesis, fluorescence, bioactivity for SHP1[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2024,265:15. |
| APA | Yan, Xue.,Zhang, Chun.,Gao, Li-Xin.,Liu, Min -Min.,Yang, Yu-Ting.,...&Wang, Wen-Long.(2024).Novel imidazo[1,2,4] triazole derivatives: Synthesis, fluorescence, bioactivity for SHP1.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,265,15. |
| MLA | Yan, Xue,et al."Novel imidazo[1,2,4] triazole derivatives: Synthesis, fluorescence, bioactivity for SHP1".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 265(2024):15. |
入库方式： OAI收割
来源：上海药物研究所
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