Coumarin-1,2,3-Triazole Conjugates as Molecular Scaffolds for the Selective Induction of ROS-Driven Apoptosis in Cancer Cells in the Development of Pyruvate Kinase M2 Inhibitors.

ABSTRACT: The increasing incidence of cancer and the emergence of drug resistance underscore the urgent need for new therapeutic options. This study aimed to synthesize and evaluate new coumarin-triazole hybrids for their cytotoxic selectivity and safety profile, providing insights into their potential as anticancer scaffolds. Twelve novel coumarin-based compounds were obtained in good yields (40-80%) and evaluated through in vitro, in silico, and in vivo assays. Among them, compound 7f displayed the highest antiproliferative potency and selectivity, with selectivity indices (SI) of 4.61 for B16F-10, 3.38 for HCT116, and 2.98 for 4T1, and an average SI of 2.18 across SCC-4, SCC-9, and SCC-25 cell lines. Mechanistic assays indicated that the cytotoxic effect of 7f i

SUBMITTER: Ouverney G 

PROVIDER: S-EPMC12750388 | biostudies-literature | 2025 Dec

REPOSITORIES: biostudies-literature