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Design, Synthesis, and Antitumor Activity Evaluation of Trifluoromethyl-Substituted Pyrimidine Derivatives Containing Urea Moiety

Russian Journal of Bioorganic Chemistry Aims and scope Submit manuscript


In order to find efficient new antitumor drugs, a series of novel pyrimidine derivatives containing urea moiety were designed and synthesized, and the antitumor activity of four human tumor cells was evaluated by MTT analysis. The results showed that most of the target compounds exhibited moderate antitumor activity. In particular, the IC50 (concentration required to achieve 50% inhibition of the tumor cell proliferation) value of compound 2-((4-(4-ethylphenoxy)-6-(trifluoromethyl)pyrimidin-2-yl)thio)-N-((4-ethylphenyl)carba-moyl)acetamide for MGC-803 (human gastric carcinoma cell line) was 2.51 ± 0.17 µmol L–1, the anti-proliferative activity was significantly better than the positive control drug 5-fluorouracil. Molecular docking revealed that this compound can bind well to the active site of epidermal growth factor receptor (EGFR), and it may become a potential antitumor drug.

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Project supported by the National Natural Science Foundation of China (no. 81773562) and this work was supported by National Key Research Program of Proteins (no. 2018YFE0195100) and Openning fund from State Key Laboratory of Esophageal Cancer Prevention & Treatment (no. K2020000X).

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Correspondence to Shan Lihong, Liu Hongmin or Zhang Qiurong.

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Liu Limin, Zhengjie, W., Xiujuan, L. et al. Design, Synthesis, and Antitumor Activity Evaluation of Trifluoromethyl-Substituted Pyrimidine Derivatives Containing Urea Moiety. Russ J Bioorg Chem 47, 1301–1311 (2021).

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