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

Add time:07/30/2019    Source:sciencedirect.com

Two new Pt(II) and Ru(II) complexes, [Pt(BFCY)Cl2] (1) and [RuCl2(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 (IC50 = 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.

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