Departamento de Química Biológica, Instituto de Química Avanzada de Cataluña (IQAC), CSIC, Jordi Girona 18-26, 08034, Barcelona, Spain.
Departamento de Química Inorgánica, Instituto de Síntesis Química y Catálisis Homogénea (ISQCH), Universidad de Zaragoza-CSIC, 50009 Zaragoza, Spain.
Bioorg Med Chem. 2022 Aug 1;67:116814. doi: 10.1016/j.bmc.2022.116814. Epub 2022 May 10.
We report four dinuclear silver(I) and gold(I) complexes containing two different bidentate N-heterocyclic carbene ligands (bisNHC). One of these complexes 4, shows strong and selective anticancer activity against the human ovarian cancer cell line A2780. Mechanistically, 4 enhances the oxidative stress by stimulating reactive oxygen species production and inhibiting the scavenging activity of thioredoxin reductase. Our findings provide evidence that tuning ligand and electronic properties of metal-NHC complexes can modulate their reactivity and selectivity and it may result in potential novel anticancer drugs.
我们报道了四个包含两种不同双齿 N-杂环卡宾配体（双 NHC）的双核银（I）和金（I）配合物。其中一个配合物 4 对人卵巢癌细胞系 A2780 表现出强烈和选择性的抗癌活性。在机制上，4 通过刺激活性氧物质的产生和抑制硫氧还蛋白还原酶的清除活性来增强氧化应激。我们的研究结果表明，调节金属-NHC 配合物的配体和电子性质可以调节其反应性和选择性，这可能导致潜在的新型抗癌药物。
