Development of coumarin and procaine linked hybrid molecules as a novel class of SHP1 fluorescent activators

IF 5.9 2区 医学 Q1 CHEMISTRY, MEDICINAL European Journal of Medicinal Chemistry Pub Date : 2025-04-15 Epub 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 ± 1.48 μM 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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香豆素和普鲁卡因结合的杂化分子作为一类新的SHP1荧光激活剂的研制
用于生物成像实验的小荧光有机分子的开发,促进了分子和细胞生物学的发展,为阐明无数细胞和多细胞过程提供了新的、有效的工具。本文首次设计合成了一类针对SHP1的荧光激活剂。代表性化合物3n对SHP1具有激活作用,EC50为17.66±1.48μM,荧光量子产率为0.521。同时,3n对SHP1具有良好的选择性,抑制了SU-DHL-2细胞和OCI-Ly10细胞的增殖,IC50分别为8.66±1.26 μM和9.16±0.53 μM,具有对人乳腺癌细胞成像的潜力。
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来源期刊
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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