3-(1H-benzoimidazol-2-yl)-chromen-2-ylideneamine platinum(II) and ruthenium(II) complexes exert their high in vitro antitumor activity by inducing S-phase arrest and disrupting mitochondrial functions in SK-OV-3/DDP tumor cells.

Graphical abstract Pt(II) complex 1- induced mitochondrial dysfunction could be an valuable target for the development of new anticancer drugs. Abstract Two new Pt(II) and Ru(II) complexes, [Pt(BFCY)Cl 2 ] (1) and [RuCl 2 (BMCY)(DMSO)] (2) with 3-(1H-benzoimidazol-2-yl)-8-fluoro-chromen-2-ylideneamine (BFCY) and 3-(1H-benzoimidazol-2-yl)-8-methyl-chromen-2-ylideneamine (BMCY), were synthesized. The BFCY Pt(II) complex 1 adopted an approximately four-coordinated square planar geometry, while BMCY complex 2 formed a distorted octahedral geometry. Among the seven selected human cancer cell lines, the two new Pt(II) and Ru(II) complexes 1 and 2 exhibited more potent activities against cisplatin-resistant SK-OV-3/DDP tumor cells (IC 50 = 2.08 ± 1.04 μM and 18.06 ± 0.36 μM, respectively), compared with the free BFCY and BMCY ligands as well as cisplatin. In addition, the BFCY Pt(II) complex 1 could induce cell cycle arrest in S phase and regulate the S-phase cell cycle-related proteins. Remarkably, the BFCY Pt(II) complex 1 also induced mitochondrial dysfunction. [ABSTRACT FROM AUTHOR]