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Abstract <p>Our research group synthesized 48 tricyclic pyrazolo[4,3-<i>d</i>]pyrimidinone compounds through a four-step process. We evaluated their inhibitory activity against human cervical cancer cells (HeLa), human colon cancer cells (HT-29), and human gastric cancer cells (HGC-27) using the MTT assay. The synthesized compounds exhibited low inhibitory activity across all three cancer cell lines, showing a marked difference in anticancer potency compared to structurally similar tricyclic pyrazolo[3,4-<i>d</i>]pyrimidinone derivatives. These results demonstrate that the position of the pyrazole ring significantly influences the physicochemical properties of tricyclic compounds, offering valuable insights for the development of novel anti-tumor lead compounds.</p>

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Synthesis and Cellular Activity Evaluation of Tricyclic Pyrazolo[4,3-d]pyrimidinones

  • 期刊论文

  • 发表日期：

    2026年6月27日

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  • Jiahao Zhou,
  • Haiqing Zhao,
  • Davron Turgunov,
  • Khurshed Bozorov,
  • Jiangyu Zhao

摘要

Abstract

Our research group synthesized 48 tricyclic pyrazolo[4,3-d]pyrimidinone compounds through a four-step process. We evaluated their inhibitory activity against human cervical cancer cells (HeLa), human colon cancer cells (HT-29), and human gastric cancer cells (HGC-27) using the MTT assay. The synthesized compounds exhibited low inhibitory activity across all three cancer cell lines, showing a marked difference in anticancer potency compared to structurally similar tricyclic pyrazolo[3,4-d]pyrimidinone derivatives. These results demonstrate that the position of the pyrazole ring significantly influences the physicochemical properties of tricyclic compounds, offering valuable insights for the development of novel anti-tumor lead compounds.