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.
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, 2026
: 202605011
.
DOI: 10.6023/cjoc202605011
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