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Synthesis, Fluorescence, and Bioactivity of Novel Isatin Derivatives

文献类型：期刊论文

作者Dong, Yi-Xin5; Gao, Li-Xin4,5; Cao, Qing5; Cao, Zi-Tong3,4; Gan, Su-Ya5; Li, Jia2,4; Zhu, Yun-Long1; Zhou, Yu-Bo2,4; Zhang, Chun5; Wang, Wen-Long5
刊名JOURNAL OF PHYSICAL CHEMISTRY B
出版日期2024-06-14
卷号128期号:25页码:6123-6133
ISSN号1520-6106
DOI10.1021/acs.jpcb.4c02561
通讯作者Zhu, Yun-Long(sequoia113847@163.com) ; Zhou, Yu-Bo(ybzhou@simm.ac.cn) ; Zhang, Chun(zhangchun@jiangnan.edu.cn) ; Wang, Wen-Long(wenlongwang@jiangnan.edu.cn)
英文摘要The isatin group is widespread in nature and is considered to be a privileged building block for drug discovery. In order to develop novel SHP1 inhibitors with fluorescent properties as tools for SHP1 biology research, this work designed and synthesized a series of isatin derivatives. The presentive compound 5a showed good inhibitory activity against SHP1(PTP) with IC50 of 11 +/- 3 mu M, displayed about 92% inhibitory rate against MV-4-11 cell proliferation at the concentration of 20 mu M, exhibited suitable fluorescent properties with a long emission wavelength and a large Stokes shift, and presented blue fluorescent imaging in HeLa cells with low cytotoxicity. This study could offer chemical tool to further understand SHP1 biology and develop novel SHP1 inhibitors in therapy.
WOS关键词PROTEIN-TYROSINE PHOSPHATASES ; IN-VITRO ; INHIBITORS ; HYBRIDS ; CELLS ; PROBE ; SHP1
资助项目National Natural Science Foundation of China[22277043] ; National Natural Science Foundation of China[JUSRP121065] ; Fundamental Research Funds for the Central Universities[JSSCBS20210848] ; High Level Personnel Project of Jiangsu Province ; BioDuro-Sundia in Wuxi and high-performance computing cluster platform of the School of Biotechnology in Jiangnan University
WOS研究方向Chemistry
语种英语
WOS记录号WOS:001248688100001
出版者AMER CHEMICAL SOC
源URL[http://119.78.100.183/handle/2S10ELR8/311932]  
专题新药研究国家重点实验室
通讯作者Zhu, Yun-Long; Zhou, Yu-Bo; Zhang, Chun; Wang, Wen-Long
作者单位1.Jiangnan Univ, Wuxi Maternal & Child Hlth Hosp, Wuxi Sch Med, Wuxi 214002, Jiangsu, Peoples R China
2.Chinese Acad Sci, Zhongshan Inst Drug Discovery, Shanghai Inst Mat Med, Zhongshan 528400, Peoples R China
3.China Pharmaceut Univ, Inst Pharmaceut Sci, Nanjing 210009, Peoples R China
4.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, State key Lab Drug Res, Shanghai 201203, Peoples R China
5.Jiangnan Univ, Sch Life Sci & Hlth Engn, Wuxi 214122, Jiangsu, Peoples R China
推荐引用方式
GB/T 7714		 Dong, Yi-Xin,Gao, Li-Xin,Cao, Qing,et al. Synthesis, Fluorescence, and Bioactivity of Novel Isatin Derivatives[J]. JOURNAL OF PHYSICAL CHEMISTRY B,2024,128(25):6123-6133.
APA Dong, Yi-Xin.,Gao, Li-Xin.,Cao, Qing.,Cao, Zi-Tong.,Gan, Su-Ya.,...&Wang, Wen-Long.(2024).Synthesis, Fluorescence, and Bioactivity of Novel Isatin Derivatives.JOURNAL OF PHYSICAL CHEMISTRY B,128(25),6123-6133.
MLA Dong, Yi-Xin,et al."Synthesis, Fluorescence, and Bioactivity of Novel Isatin Derivatives".JOURNAL OF PHYSICAL CHEMISTRY B 128.25(2024):6123-6133.

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来源：上海药物研究所

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