Abstract
Two new quinolone ruthenium(II)-arene complexes, i.e., [Ru(cym)(DClQ)] (Ru1) and [Ru(cym)(ClQ)] (Ru2), with 5,7-dichloro-8-hydroxyquinoline (H-DClQ), 5-chloro-8-hydroxyquinoline (H-ClQ) and [(η6-p-cymene)RuI2]2 (cym), were first designed. The cytotoxic activity of two new quinolone Ru(II)-arene complexes Ru1 and Ru2 has been evaluated in T-24 bladder carcinoma, Hep-G2 hepatoma, BEL-7404 hepatocellular carcinoma, MGC80-3 gastric adenocarcinoma, and non-tumorous HL-7702 liver cells in order to study structure-activity relationships of their anti-tumor activity. Additionally, the cytotoxic activity of quinolone Ru(II)-arene complex Ru1 was much higher potent than Ru2 and cisplatin, with low IC50 values was 0.02 ± 0.0.1 μM against T-24 bladder carcinoma cells. The mechanism studies testified that quinolone Ru(II)-arene complexes Ru1 and Ru2 induced apoptosis in T-24 bladder carcinoma cells by generating ROS metabolites, triggering caspase-9 increase and mitochondrial membrane potential loss. The quinolone Ru(II)-arene complex Ru1 with 5,7-dichloro-8-hydroxyquinoline (H-DClQ) ligand was considerably more active than the 5-chloro-8-hydroxyquinoline Ru2 complex.
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