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Design, synthesis and anti-tumor activity evaluation of 4,6,7-substitute quinazoline derivatives

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Abstract

A series of novel 4,6,7-substituted quinazoline derivatives were designed, synthesized and evaluated for their antiproliferative activities against human cancer cell lines (PC-3, MGC-803, HGC-27, A549 and H1975). Among all the target compounds, compound 22s displayed the most potent anti-proliferative activity against MGC-803 cells in vitro. Further mechanism studies revealed that compound 22s could obviously inhibit the colony formation and migration of MGC-803 cells. At the same time, compound 22s could induced apoptosis of MGC-803 cells and induced cell cycle arrest at G1-phase. Collectively, those work suggested that compound 22s might be a valuable solution to optimize anilinoquinazoline-based antineoplastic agents.

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Acknowledgements

This work was supported by the National Natural Science Foundation of China (No. U1904163).

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Authors and Affiliations

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

    Honglin Dai, Xiaojie Si, Hao Wang, Lingling Chi, Chao Gao, Zhengjie Wang, Limin Liu, Zhuo Qian, Yu Ke, Qiurong Zhang & Hongmin Liu

  2. Collaborative Innovation Center of New Drug Research and Safety Evaluation of Henan Province, 450001, Zhengzhou, China

    Honglin Dai, Xiaojie Si, Hao Wang, Lingling Chi, Chao Gao, Zhengjie Wang, Limin Liu, Zhuo Qian, Yu Ke, Qiurong Zhang & Hongmin Liu

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

    Yu Ke, Qiurong Zhang & Hongmin Liu

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

    Yu Ke, Qiurong Zhang & Hongmin Liu

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  1. Honglin Dai
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  2. Xiaojie Si
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Correspondence to Yu Ke, Qiurong Zhang or Hongmin Liu.

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Dai, H., Si, X., Wang, H. et al. Design, synthesis and anti-tumor activity evaluation of 4,6,7-substitute quinazoline derivatives. Med Chem Res 31, 1351–1368 (2022). https://doi.org/10.1007/s00044-022-02897-9

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  • DOI: https://doi.org/10.1007/s00044-022-02897-9

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