Department of Chemical Engineering, Faculty of Engineering, Ardakan University, P.O. Box 184, Ardakan, Iran.
School of Chemistry, National University of Ireland, Galway, University Road, Galway, H91 TK33, Ireland.
Biometals. 2020 Jun;33(2-3):107-122. doi: 10.1007/s10534-020-00235-3. Epub 2020 Apr 3.
A new cyclometalated Au(III) complex highlighting a naphthoquinone-C^N scaffold with formula (NQ-N^C)Au(SAd)Cl, 1, in which NQ-N^C: 2-(5-amino-benzo[h]quinolone)-3-(3-methyl-2-butenyl)-1,4-naphthoquinone, HSAd: 1-adamantanethiol, was synthesized and characterized. The interaction of complex 1 with cysteine (CysH) was experimentally and theoretically studied. Complex 1 was more active against MCF-7 and A549 cancer cell lines and less active in a healthy cell (non-tumorigenic cells, MRC-5) than cisplatin. The DNA binding and inhibition of thioredoxin reductase of complex 1 were studied and compared with the molecular docking results. The generation of reactive oxygen species (ROS) and apoptosis of this new complex were also investigated.
一种新型的金属环戊二烯基金（III）配合物，突出了萘醌-C^N 骨架，其化学式为（NQ-N^C）Au（SAd）Cl，1，其中 NQ-N^C：2-（5-氨基苯并[h]喹啉酮）-3-（3-甲基-2-丁烯基）-1,4-萘醌，HSAd：1-金刚烷硫醇，被合成并进行了表征。配合物 1 与半胱氨酸（CysH）的相互作用进行了实验和理论研究。与顺铂相比，配合物 1 对 MCF-7 和 A549 癌细胞系的活性更高，对健康细胞（非致瘤细胞，MRC-5）的活性更低。研究了配合物 1 的 DNA 结合和硫氧还蛋白还原酶抑制作用，并与分子对接结果进行了比较。还研究了这种新配合物的活性氧（ROS）的产生和细胞凋亡。
