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Article

Scaffold-Hopping Design and Synthesis of Thieno[3,2-d]pyrimidines: Anticancer Activity, Apoptosis Induction, and In Silico Inhibition of CDKs

by
Zukela Ruzi
1,2,
Anvarjon Buronov
3,
Lifei Nie
1,*,
Azizbek Nasrullaev
3,
Zarifa Murtazaeva
3,
Rustamkhon Kuryazov
4,
Jiangyu Zhao
1,
Thomas Efferth
5,
Haji Akber Aisa
1 and
Khurshed Bozorov
1,3,*
1
State 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, China
2
School of Chemistry and Chemical Engineering, Changji University, Changji 831100, China
3
Department of Organic Synthesis and Bioorganic Chemistry, Institute of Biochemistry, Samarkand State University, University Blvd. 15, Samarkand 140104, Uzbekistan
4
Department of Chemistry, Urgench State University, Kh. Olimjon st. 14, Urgench 220100, Uzbekistan
5
Department of Pharmaceutical Biology, Institute of Pharmaceutical and Biomedical Sciences, Johannes Gutenberg University, Staudinger Weg 5, 55128 Mainz, Germany
*
Authors to whom correspondence should be addressed.
Int. J. Mol. Sci. 2025, 26(17), 8528; https://doi.org/10.3390/ijms26178528
Submission received: 14 July 2025 / Revised: 12 August 2025 / Accepted: 27 August 2025 / Published: 2 September 2025
(This article belongs to the Special Issue Sulfur-Containing Compounds: Synthesis, Characterization and Antimicrobial or Anticancer Activity)
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Abstract

Two series of tricyclic thieno[3,2-d]pyrimidines were synthesized, achieving yields of up to 97%. The tricyclic thieno[3,2-d]pyrimidines examined in this study are synthetic analogs of the deoxyvasicinone alkaloids, where the thiophene ring substitutes for the benzene ring. A systematic investigation was conducted on the scaffold-hopping strategy of these alkaloids, emphasizing the selective synthesis and anticancer properties of thieno[3,2-d]pyrimidines. The anticancer evaluation was performed on human cancer cell lines, specifically cervical HeLa and colon HT-29 carcinoma cells. Additional bioassays included cell migration analyses, cell cycle progression, apoptosis, and molecular docking analyses. Furthermore, molecular docking studies showed that the most active small molecule 6e is likely to disrupt the cell cycle process through targeting CDKs (Cyclin-dependent kinases), leading to the inhibition of tumor cell proliferation.
Keywords: anticancer activity; apoptosis induction; cell cycle arrest; cyclin-dependent kinases (CDKs); CDK1; in silico study; molecular docking; scaffold-hopping synthesis; thieno[3,2-d]pyrimidines anticancer activity; apoptosis induction; cell cycle arrest; cyclin-dependent kinases (CDKs); CDK1; in silico study; molecular docking; scaffold-hopping synthesis; thieno[3,2-d]pyrimidines
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MDPI and ACS Style

Ruzi, Z.; Buronov, A.; Nie, L.; Nasrullaev, A.; Murtazaeva, Z.; Kuryazov, R.; Zhao, J.; Efferth, T.; Aisa, H.A.; Bozorov, K. Scaffold-Hopping Design and Synthesis of Thieno[3,2-d]pyrimidines: Anticancer Activity, Apoptosis Induction, and In Silico Inhibition of CDKs. Int. J. Mol. Sci. 2025, 26, 8528. https://doi.org/10.3390/ijms26178528

AMA Style

Ruzi Z, Buronov A, Nie L, Nasrullaev A, Murtazaeva Z, Kuryazov R, Zhao J, Efferth T, Aisa HA, Bozorov K. Scaffold-Hopping Design and Synthesis of Thieno[3,2-d]pyrimidines: Anticancer Activity, Apoptosis Induction, and In Silico Inhibition of CDKs. International Journal of Molecular Sciences. 2025; 26(17):8528. https://doi.org/10.3390/ijms26178528

Chicago/Turabian Style

Ruzi, Zukela, Anvarjon Buronov, Lifei Nie, Azizbek Nasrullaev, Zarifa Murtazaeva, Rustamkhon Kuryazov, Jiangyu Zhao, Thomas Efferth, Haji Akber Aisa, and Khurshed Bozorov. 2025. "Scaffold-Hopping Design and Synthesis of Thieno[3,2-d]pyrimidines: Anticancer Activity, Apoptosis Induction, and In Silico Inhibition of CDKs" International Journal of Molecular Sciences 26, no. 17: 8528. https://doi.org/10.3390/ijms26178528

APA Style

Ruzi, Z., Buronov, A., Nie, L., Nasrullaev, A., Murtazaeva, Z., Kuryazov, R., Zhao, J., Efferth, T., Aisa, H. A., & Bozorov, K. (2025). Scaffold-Hopping Design and Synthesis of Thieno[3,2-d]pyrimidines: Anticancer Activity, Apoptosis Induction, and In Silico Inhibition of CDKs. International Journal of Molecular Sciences, 26(17), 8528. https://doi.org/10.3390/ijms26178528

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