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Novel ruthenium azo-quinoline complexes with enhanced photonuclease activity in human cancer cells
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2017-08-26 , DOI: 10.1016/j.ejmech.2017.08.059
Mangesh H. Kaulage , Basudeb Maji , Sanjeev Pasadi , Santanu Bhattacharya , K. Muniyappa

Coordinatively saturated ruthenium complexes with a variable net charge are currently under intense investigation for their anticancer potential. These complexes, possessing long wavelength metal-to-ligand charge transfer with DNA photonuclease activity, have shown promising cytotoxic profiles. Although most of the ruthenium complexes exhibit significant photochemotherapeutic activity, their poor entry into cells hinder their development as potential drug molecules. Here, we report the synthesis and characterization of four new ruthenium (II) azo-8-hydroxyquinoline complexes, their mode of in vitro DNA binding and antiproliferative properties against cultured human cancer cell lines. The activity of these compounds prior to photoirradiation is minimal. However, they could induce DNA photonuclease activity through the generation of reactive oxygen species upon exposure to light. The activities exhibited by these complexes were found to be more efficient (>5-fold) than cisplatin, emphasizing their therapeutic potential. Collectively, these results support the idea that ruthenium (II) azo-8-hydroxyquinoline complexes can serve as potential agents in photodynamic anticancer therapy.



中文翻译:

新型钌偶氮喹啉络合物在人类癌细胞中具有增强的光核酸酶活性

具有可变净电荷的配位饱和钌配合物目前正在深入研究其抗癌潜力。这些复合物具有长波长的金属到配体的电荷转移以及DNA光核酸酶的活性,显示出令人鼓舞的细胞毒性特征。尽管大多数钌配合物表现出显着的光化学治疗活性,但它们进入细胞的不良进入阻碍了其作为潜在药物分子的发展。在这里,我们报告的合成和表征的四个新的钌(II)偶氮8-羟基喹啉配合物,其体外模式针对培养的人类癌细胞系的DNA结合和抗增殖特性。这些化合物在光辐照之前的活性是最小的。但是,它们可以通过在暴露于光线下产生活性氧来诱导DNA光核酸酶活性。发现这些复合物表现出的活性比顺铂更有效(> 5倍),强调了它们的治疗潜力。总体而言,这些结果支持了钌(II)偶氮8-羟基喹啉络合物可以作为光动力抗癌治疗中的潜在药物的想法。

更新日期:2017-08-26
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