Vellé Alba, Maguire Ronan, Kavanagh Kevin, Sanz Miguel Pablo J, Montagner Diego
Departamento de Química Inorgánica, Instituto de Síntesis Química y Catálisis Homogénea, ISQCH, Universidad de Zaragoza-CSIC, 50009, Zaragoza, Spain.
Chemistry Department, Maynooth University, Maynooth, Ireland.
ChemMedChem. 2017 Jun 7;12(11):841-844. doi: 10.1002/cmdc.201700257. Epub 2017 May 19.
A series of gold(I) pioneer complexes bearing N-heterocyclic carbenes and steroid derivatives (ethynylestradiol and ethisterone) with the generic formula [Au(R -imidazol-2-ylidene)(steroid)] (where R=CH or CH CH OCH ) were synthesized, and the X-ray structure of a rare of gold(I)-estradiol derivative is discussed. Toxicity studies reveal notable antibacterial activity of the gold-based compounds, which is significantly increased in vivo by the presence of the estradiol unit. Toxicity profiling was estimated in vitro versus Gram-positive (Staphylococcus aureus) and Gram-negative (Escherichia coli) bacteria, and in vivo on Galleria mellonella larvae against E. coli.
合成了一系列通式为[Au(R -咪唑-2-亚基)(甾体)]（其中R = CH或CH CH OCH ）的含N-杂环卡宾和甾体衍生物（乙炔雌二醇和炔诺酮）的金（I）先导配合物，并讨论了一种罕见的金（I）-雌二醇衍生物的X射线结构。毒性研究表明，这些金基化合物具有显著的抗菌活性，在体内，由于雌二醇单元的存在，其抗菌活性显著增强。对革兰氏阳性菌（金黄色葡萄球菌）和革兰氏阴性菌（大肠杆菌）进行了体外毒性分析，并在体内对大蜡螟幼虫针对大肠杆菌进行了毒性分析。
