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Design, synthesis and antitumor activity evaluation of 5-cyano-2,4,6-substituted pyrimidine derivatives containing acrylamide group

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Abstract

A series of novel 5-cyano-2,4,6-substituted pyrimidine derivatives containing acrylamide group were designed, synthesized, and evaluated for their antitumor activity against four human cancer cell lines (MGC-803, PC-3, A549, and H1975) using the MTT assay. Among them, compound 20y exhibited the most potent cytotoxicity against PC-3 cells (IC50 = 2.75 ± 0.08 μM). Notably, compound 20y significantly inhibited the colony formation, migration, and invasion of PC-3 cells. Furthermore, compound 20y induced S-phase cell cycle arrest and apoptosis in PC-3 cells. These findings indicate that compound 20y might serve as a valuable lead compound for developing antitumor agents targeting prostate cancer cells.

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Acknowledgements

This work was supported by the National Natural Science Foundation of China (No. U21A20416).

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Authors and Affiliations

  1. School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, 450001, China

    Fuqiang Yu, Lingling Chi, Hao Wang, Chao Gao, Honglin Dai, Limin Liu, Zhengjie Wang, Yu Ke, Hongmin Liu & Qiurong Zhang

  2. Institute of Drug Discovery and Development, Zhengzhou, 450001, China

    Fuqiang Yu, Lingling Chi, Hao Wang, Chao Gao, Honglin Dai, Limin Liu, Zhengjie Wang, Hongmin Liu & Qiurong Zhang

  3. State Key Laboratory of Esophageal Cancer Prevention & Treatment, Zhengzhou, 450052, China

    Yu Ke, Hongmin Liu & Qiurong Zhang

  4. Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education, Zhengzhou, 450001, China

    Yu Ke, Hongmin Liu & Qiurong Zhang

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  1. Fuqiang Yu
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Yu, F., Chi, L., Wang, H. et al. Design, synthesis and antitumor activity evaluation of 5-cyano-2,4,6-substituted pyrimidine derivatives containing acrylamide group. Med Chem Res 32, 2116–2124 (2023). https://doi.org/10.1007/s00044-023-03099-7

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