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Combining [Arene-Ru] with Azocarboxamide to Generate a Complex with Cytotoxic Properties

机译:[Arene-Ru]与偶氮酰胺结合生成具有细胞毒性的复合物

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Azocarboxamide (azcH) has been combined for the first time with [Ru-Cym] to generate metal complexes with N,N- and N,O-coordination mode, [(Cym) Ru(azc)Cl] and [(Cym) Ru(azcH) Cl](+)[PF6](-). Geometric and electronic structures of the complexes are reported along with their in vitro activities against different tumour cell lines and preliminary results on solution chemistry. Compound [(Cym) Ru(azc)Cl] exhibited remarkable cytotoxic properties. It was cell-type specific and had comparable IC50 values towards both cancer cells and their drug-resistant subline. A tenfold increase in the sensitivity towards [(Cym) Ru(azc)Cl] was noted for the tumour cells with depleted intracellular glutathione (GSH) level, suggesting the essential role of GSH in cell response to this compound.
机译:偶氮羧酰胺(azcH)首次与[Ru-Cym]结合生成具有N,N-和N,O配位模式[[Cym)Ru(azc)Cl]和[(Cym)Ru的金属配合物(azcH)Cl](+)[PF6](-)。报道了配合物的几何和电子结构,以及它们针对不同肿瘤细胞系的体外活性以及溶液化学的初步结果。化合物[(Cym)Ru(azc)Cl]表现出显着的细胞毒性。它具有细胞类型特异性,并且对癌细胞及其耐药亚系具有可比的IC50值。对于具有耗尽的细胞内谷胱甘肽(GSH)水平的肿瘤细胞,对[(Cym)Ru(azc)Cl]的敏感性提高了十倍,这表明GSH在细胞对该化合物的反应中起着至关重要的作用。

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