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Synthesis, fluorescence properties of novel thiazolo[3,2-b][1,2,4]triazol derivatives as potent SHP2 inhibitors and its uses in sensing for Fe3+and cell imaging

文献类型：期刊论文

作者Yan, Xue1,4; Zhang, Chun1; Gao, Li-Xin3; Cao, Zi-Tong3,6; Gan, Su-Ya1; Li, Jia2; Xiang, Da-Jun5; Zhou, Yu-Bo2; Wang, Wen-Long1,4
刊名JOURNAL OF MOLECULAR STRUCTURE
出版日期2025-03-05
卷号1324页码:12
关键词Thiazolo[3,2-b][1,2,4]triazole Salicylic acid Fe3+ion Fluorescence property SHP2
ISSN号0022-2860
DOI10.1016/j.molstruc.2024.140960
通讯作者Xiang, Da-Jun(xiangdjxshospital@yeah.net) ; Zhou, Yu-Bo(ybzhou@simm.ac.cn) ; Wang, Wen-Long(wenlongwang@jiangnan.edu.cn)
英文摘要A series of thiazolo[3,2-b][1,2,4]triazole derivatives containing salicylic acid fragment were designed and synthesized. Then, their optical properties and biological activities were evaluated. Among them, the representative compound 5-2k exhibited higher selectivity/specificity for Fe3+, a low limit of detection (LOD) of 8.2 mu M and moderate inhibitory activity against SHP2 with IC50 of 2.85 +/- 0.50 mu M. Moreover, the activities of SHP1, SHP2, PTP1B and TCPTP enzyme could be adjusted effectively through the interaction between compound 5-2k and metal ion Fe3+. Furthermore, compound 5-2k had low cytotoxicity for peripheral blood mononuclear cell (PBMC) and excellent blue signal in HeLa cell imaging. These results are expected to facilitate the development of novel sensitive and specific fluorescence sensors for Fe3+ and SHP2 inhibitor for cancer therapy.
WOS关键词SMALL-MOLECULE INHIBITOR ; SALICYLIC-ACID ; IRON(III) IONS ; IRON IONS ; TYROSINE ; SENSOR ; CANCER ; COPPER ; PROBE ; HPLC
资助项目National Natural Science Foundation of China[22277043] ; Fundamental Research Funds for the Central Universities[JUSRP121065] ; High Level Personnel Project of Jiangsu Province[JSSCBS20210848]
WOS研究方向Chemistry
语种英语
WOS记录号WOS:001373097800001
出版者ELSEVIER
源URL[http://119.78.100.183/handle/2S10ELR8/315010]  
专题中国科学院上海药物研究所
通讯作者Xiang, Da-Jun; 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.Chinese Acad Sci, Zhongshan Inst Drug Discovery, Shanghai Inst Mat Med, SSIP Healthcare & Med Demonstrat Zone, Zhongshan 528400, Peoples R China
3.Chinese Acad Sci, Shanghai Inst Mat Med, Stake Key Lab Chem Biol, Shanghai 201203, Peoples R China
4.Jiangnan Univ, Sch Chem & Mat Engn, Wuxi 214122, Jiangsu, Peoples R China
5.Xishan Peoples Hosp Wuxi City, Wuxi 214105, Jiangsu, Peoples R China
6.China Pharmaceut Univ, Inst Pharmaceut Sci, Nanjing 210009, Jiangsu, Peoples R China
推荐引用方式
GB/T 7714		 Yan, Xue,Zhang, Chun,Gao, Li-Xin,et al. Synthesis, fluorescence properties of novel thiazolo[3,2-b][1,2,4]triazol derivatives as potent SHP2 inhibitors and its uses in sensing for Fe3+and cell imaging[J]. JOURNAL OF MOLECULAR STRUCTURE,2025,1324:12.
APA Yan, Xue.,Zhang, Chun.,Gao, Li-Xin.,Cao, Zi-Tong.,Gan, Su-Ya.,...&Wang, Wen-Long.(2025).Synthesis, fluorescence properties of novel thiazolo[3,2-b][1,2,4]triazol derivatives as potent SHP2 inhibitors and its uses in sensing for Fe3+and cell imaging.JOURNAL OF MOLECULAR STRUCTURE,1324,12.
MLA Yan, Xue,et al."Synthesis, fluorescence properties of novel thiazolo[3,2-b][1,2,4]triazol derivatives as potent SHP2 inhibitors and its uses in sensing for Fe3+and cell imaging".JOURNAL OF MOLECULAR STRUCTURE 1324(2025):12.

入库方式： OAI收割

来源：上海药物研究所

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