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Thieno[3,2-d]pyrimidines in Anticancer Drug Discovery: Recent Advances in Drug Design and Molecular Targets

Anvarjon BuronovDepartment of Medicinal Chemistry, Institute of Biochemistry, Samarkand State University, University Blvd. 15, Samarkand 140104, UzbekistanShukhrat GaybullaevDepartment of Medicinal Chemistry, Institute of Biochemistry, Samarkand State University, University Blvd. 15, Samarkand 140104, UzbekistanZarifa MurtazaevaDepartment of Medicinal Chemistry, Institute of Biochemistry, Samarkand State University, University Blvd. 15, Samarkand 140104, UzbekistanFeruza RuzievaDepartment of Medicinal Chemistry, Institute of Biochemistry, Samarkand State University, University Blvd. 15, Samarkand 140104, UzbekistanZohidjon KhushnazarovDepartment of Medicinal Chemistry, Institute of Biochemistry, Samarkand State University, University Blvd. 15, Samarkand 140104, UzbekistanDavron TurgunovDepartment of Medicinal Chemistry, Institute of Biochemistry, Samarkand State University, University Blvd. 15, Samarkand 140104, UzbekistanAzizbek NasrullaevDepartment of Medicinal Chemistry, Institute of Biochemistry, Samarkand State University, University Blvd. 15, Samarkand 140104, UzbekistanRustamkhon KuryazovDepartment of Chemistry, Urgench State University named after Abu Rayhan Biruni, Kh. Olimjon st. 14, Urgench 220100, UzbekistanYu. R. TakhirovDepartment of Chemistry, Urgench State University named after Abu Rayhan Biruni, Kh. Olimjon st. 14, Urgench 220100, UzbekistanFirdavsi TursunovDepartment of Medicinal Chemistry, Institute of Biochemistry, Samarkand State University, University Blvd. 15, Samarkand 140104, UzbekistanTemur KushatovDepartment of Medicinal Chemistry, Institute of Biochemistry, Samarkand State University, University Blvd. 15, Samarkand 140104, UzbekistanDushamov Dilshod AzadovichDepartment of Chemistry, Urgench State University named after Abu Rayhan Biruni, Kh. Olimjon st. 14, Urgench 220100, UzbekistanShavkat MatmuratovDepartment of Chemistry, Urgench State University named after Abu Rayhan Biruni, Kh. Olimjon st. 14, Urgench 220100, UzbekistanNilufar NurullaevaDepartment of Chemistry, Urgench State University named after Abu Rayhan Biruni, Kh. Olimjon st. 14, Urgench 220100, UzbekistanAziza ShodikulovaSamarkand State Medical University, Amir Temur st. 18, Samarkand 140100, UzbekistanKakhor KhalikovSamarkand State Medical University, Amir Temur st. 18, Samarkand 140100, UzbekistanDilafruz KholmurodovaScientific and Practical Center of Immunology, Allergology and Human Genomics, Samarkand State Medical University, Makhdūm-i Aʿẓam st. 18, Samarkand 140104, UzbekistanSodik NumonovResearch Institution “Chinese-Tajik Innovation Center for Natural Products”, National Academy of Sciences of Tajikistan, Dushanbe 734063, TajikistanChao NiuState Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, South Beijing Rd 40-1, Urumqi 830011, ChinaYuanyuan JiDepartment of Geriatric General Surgery, The Second Affiliated Hospital, Xi’an Jiaotong University, Xi’an 710004, ChinaJiangyu ZhaoXinjiang Technical Institute of Physics & ChemistryZhishen GeSchool of Chemistry, State Key Laboratory of Fluorine & Nitrogen Chemicals, Institute of New Concept Sensors and Molecular Materials (INCSMM), Engineering Research Center of Energy Storage Materials and Devices, Ministry of Education, Xi’an Key Laboratory of Sustainable Polymer Materials, Xi’an Jiaotong University, Xi’an 710049, ChinaKhurshed BozorovDepartment of Medicinal Chemistry, Institute of Biochemistry, Samarkand State University, University Blvd. 15, Samarkand 140104, Uzbekistan

2026en

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The thieno[3,2-d]pyrimidine scaffolds have emerged as an important class of heterocycles in anticancer drug discovery, with clinically advanced drugs olmutinib and pictilisib highlighting their therapeutic potential. This review presents thieno[3,2-d]pyrimidine-containing anticancer agents reported between January 2008 and August 2025, focusing on synthetic methodologies, anticancer-related biological activities, and structure–activity relationships. Thieno[3,2-d]pyrimidine derivatives have been investigated as inhibitors of numerous cancer-related targets, including EGFR, PI3K/mTOR, CDKs, JAK, VEGFR, HDAC, ATR, and other oncogenic proteins. This review also summarizes thieno[3,2-d]pyrimidine scaffolds with anticancer activity, with particular emphasis on the design and synthesis of lead compounds, molecular hybridization strategies, and recent advances in this area. Synthetic pathways for lead compounds are systematically presented and discussed, along with pharmacophoric features. In addition, detailed structure–activity relationship analyses are provided to highlight the influence of heterocyclic fusion, linker optimization, hydrogen-bonding motifs, electronic effects, hydrophobic fragments, and the introduction of hybrid scaffolds on antiproliferative potency, kinase inhibition, selectivity, and multitarget activity. In addition, this review demonstrates the significant potential of thieno[3,2-d]pyrimidine-based scaffolds as a privileged platform for the development of next-generation targeted anticancer agents and offers valuable guidance for future medicinal chemistry research.

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DOI: 10.3390/ijms27167457

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