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

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 sm

SUBMITTER: Ruzi Z 

PROVIDER: S-EPMC12429047 | biostudies-literature | 2025 Sep

REPOSITORIES: biostudies-literature