Abstract
New glycoside-prodrugs based on the iron chelator deferasirox were designed. Selective enzymatic activation by glycosidases was observed within 24 hours, accompanied by cancer cell-selective cytotoxicity. Notably, derivative 3a, bearing a β-d-galactose moiety, showed promising selective activity against galactosidase overexpressing OvCar-3 cells (IC(50) 9.1 ± 1.6 μM) while maintaining low activity against fibroblast control GM5756 cells (IC(50) > 100 μM).