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

Jiahao ZhouState Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, 830011, Urumqi, ChinaHaiqing ZhaoState Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, 830011, Urumqi, ChinaDavron TurgunovDepartment of Organic Synthesis and Bioorganic Chemistry, Institute of Biochemistry, Samarkand State University, 140104, Samarkand, UzbekistanK h A BozorovXinjiang Technical Institute of Physics & ChemistryJ Z ZhaoUniversity of Chinese Academy of Sciences

2026en

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Annotatsiya

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.

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DOI: 10.1134/s1070363226600153

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