Synthesis and Biological Activity of Novel 5-Fluoropyrimidin Containing Isoindolin-1-One

doi:10.6023/cjoc202605011

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含异吲哚酮的5-氟嘧啶衍生物的合成及生物活性研究

曹瑞霞^a,*, 贾玉萍^b, 董欣雨^a, 张礼蓉^a, 李明瑞^a, 王安琪^a, 庞琳茹^a, 吴金璇^a

^a齐鲁师范学院化学与化工学院济南 250200;
^b山东省药学科学院济南 250101

收稿日期:2026-05-13 修回日期:2026-06-26
基金资助:
齐鲁师范学院青年博士支持计划(No. QBJH19-0038)、国家自然科学基金面上项目(Nos. 82372242, 82272324, 22477142)资助

Synthesis and Biological Activity of Novel 5-Fluoropyrimidin Containing Isoindolin-1-One

Cao Ruixia^a,*, Jia Yuping^b, Dong Xinyu^a, Zhang Lirong^a, Li Mingrui^a, Wang Anqi^a, Pang Linru^a, Wu Jinxuan^a

^aCollege of Chemistry and Chemical Engineering, Qilu Normal University, Jinan, 250200;
^bShandong Academy of pharmaceutical Sciences, Jinan, 250101

Received:2026-05-13 Revised:2026-06-26
Contact: *E-mail: crx0510@163.com
Supported by:
Young Doctor Support Program of Qilu Normal University (No. QBJH19-0038) and National Natural Science Foundation of China (Nos. 82372242, 82272324, 22477142)

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Abstract

In order to search for new structural anti-tumor drugs, a series of novel 5-fluoropyrimidin derivatives containing isoindolin-1-one were synthesized for the first time and evaluated for their inhibitory activities against B lymphocyte(Raji), Human breast cancer cell(MCF-7), Human hepatoma carcinoma cells(HepG2), mouse B lymphoma(A20) and Human colon cancer cell(HCT116) by using MTT assay. 16 compounds reported herein were new compounds, these chemical structures were well characterized by nuclear magnetic resonance spectroscopy (NMR) and high-resolution mass spectra (HRMS) spectroscopic methods. Compound 6a showed the most potent inhibitory activity against Raji cells with the IC₅₀ values of 1.56 μmol/L, compound 6j showed the most potent inhibitory activity against A20 cells, IC₅₀ values of 0.99 μmol/L, compound 6j showed the most potent inhibitory activity against HCT116 cells with the IC₅₀ values of 3.21 μmol/L, they were better than Fostamatinib. Compound 6l showed the most potent inhibitory activity against MCF-7 cells with the IC₅₀ values of 14.28 μmol/L than Palbociclib. Compound 6j showed the most potent inhibitory activity against HepG2 cells with the IC₅₀ values of 5.01 μmol/L than Sorafenib tosylate.

Key words: 5-Fluoropyrimidin, Synthesis, Anticancer, Molecular docking, Structure-activity relationship

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Cao Ruixia, Jia Yuping, Dong Xinyu, Zhang Lirong, Li Mingrui, Wang Anqi, Pang Linru, Wu Jinxuan. Synthesis and Biological Activity of Novel 5-Fluoropyrimidin Containing Isoindolin-1-One[J]. Chinese Journal of Organic Chemistry, doi: 10.6023/cjoc202605011.

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含异吲哚酮的5-氟嘧啶衍生物的合成及生物活性研究

Synthesis and Biological Activity of Novel 5-Fluoropyrimidin Containing Isoindolin-1-One

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