Design, synthesis and evaluation of fluorescent dihydropyridine-dihydropyrimidinone hybrids as inducers of cell-cycle arrest in a prostate cancer cell line <i>via</i> Aurora kinase interactions.

ABSTRACT: Fluorescent dihydropyridine-dihydropyrimidinone (DHP-DHPM) hybrids were easily synthesized through the combination of Hantzsch and Biginelli multicomponent reactions followed by a copper-catalyzed azide-alkyne cycloaddition reaction (CuAAC, click chemistry) protocol. Nine hybrids showed promising antitumor activity for the PC3 prostate cancer cell line, notably compounds 9d and 9g. Both hybrids exhibited high selectivity for tumor cells, with significant selectivity indices (SI), particularly 9g (SI >68.8). Selectivity was qualitatively observed by the internalization of the fluorescent hybrids through high-resolution confocal laser scanning microscopy (CLSM). In silico investigations and western blotting analysis showed a selective inhibition of the isoform C of Aurora kinase by hy

SUBMITTER: de Souza VP 

PROVIDER: S-EPMC12530137 | biostudies-literature | 2025 Sep

REPOSITORIES: biostudies-literature