Development of Coumarin and Procaine Linked Hybrid Molecules as A Novel Class of SHP1 Fluorescent Activators

IF 6 2区 医学 Q1 CHEMISTRY, MEDICINAL European Journal of Medicinal Chemistry Pub Date : 2025-02-17 DOI:10.1016/j.ejmech.2025.117394
Xu-Yang Mu, Li-Xin Gao, Zhen-Xuan Zhang, Zi-Tong Cao, Qing Cao, Chun Zhang, Jia Li, Da-Jun Xiang, Yu-Bo Zhou, Wen-Long Wang
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Abstract

The development of small fluorescent organic molecules used in bioimaging experiment has boomed the progress of molecular and cellular biology, providing new and efficient tools to elucidate a myriad of cellular and multicellular processes. In this work, a class of fluorescent activators against SHP1 was designed and synthesized for the first time. The representative compound 3n showed activating effect against SHP1 with EC50 of 17.66 ± 1.48μM and a fluorescence quantum yield of 0.521 in DMSO. Meanwhile, 3n showed good selectivity for SHP1, inhibited the proliferation of SU-DHL-2 cells and OCI-Ly10 cells with IC50 of 8.66 ± 1.26 μM and 9.16 ± 0.53 μM and exhibited potential for cellular imaging on human breast cancer cells.

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CiteScore
11.70
自引率
9.00%
发文量
863
审稿时长
29 days
期刊介绍: The European Journal of Medicinal Chemistry is a global journal that publishes studies on all aspects of medicinal chemistry. It provides a medium for publication of original papers and also welcomes critical review papers. A typical paper would report on the organic synthesis, characterization and pharmacological evaluation of compounds. Other topics of interest are drug design, QSAR, molecular modeling, drug-receptor interactions, molecular aspects of drug metabolism, prodrug synthesis and drug targeting. The journal expects manuscripts to present the rational for a study, provide insight into the design of compounds or understanding of mechanism, or clarify the targets.
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Editorial Board Contents continued Graphical abstract TOC Graphical abstract TOC In silico modeling of targeted protein degradation
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