Hackenberg F, Tacke M
University College Dublin, Belfield, Dublin 4, Ireland.
Dalton Trans. 2014 Jun 14;43(22):8144-53. doi: 10.1039/c4dt00624k. Epub 2014 Apr 28.
Benzyl-substituted metallocarbene compounds synthesised by our group and others during the past 5 years give a new perspective on their activity as antibiotic and antitumoral drugs. N-heterocyclic carbenes containing an imidazole core were functionalised and their transition metal complexes (M = Ag, Au, Cu, Ru) have shown promising antibacterial as well as anticancer activity in vitro and in vivo. IC50 values in the nanomolar region or antibacterial activity comparable to conventional antibiotics lead the way towards novel drug candidates.
在过去5年里，我们团队及其他团队合成的苄基取代金属卡宾化合物，为其作为抗生素和抗肿瘤药物的活性提供了新视角。含有咪唑核心的N-杂环卡宾被官能化，其过渡金属配合物（M = Ag、Au、Cu、Ru）在体外和体内均显示出有前景的抗菌和抗癌活性。纳摩尔区域的IC50值或与传统抗生素相当的抗菌活性，为新型候选药物指明了方向。
