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Synthesis, characterization, and antileishmanial activity of neutral N-heterocyclic carbenes gold(I) complexes
European Journal of Medicinal Chemistry ( IF 6.7 ) Pub Date : 2017-10-24 , DOI: 10.1016/j.ejmech.2017.10.060
Chen Zhang , Sandra Bourgeade Delmas , Álvaro Fernández Álvarez , Alexis Valentin , Catherine Hemmert , Heinz Gornitzka

A series of five new mononuclear neutral gold(I) complexes containing N-heterocyclic carbenes (NHCs) was synthesized and fully characterized by spectroscopic methods. The X-ray structures of four complexes are presented. These gold(I) complexes together with four other neutral gold(I)-NHC complexes previously described were evaluated in vitro against Leishmania infantum promastigotes and axenic amastigotes. Moreover, their cytotoxicity was assessed on the murine macrophages J774A.1. Except one complex (10), eight gold(I)-NHC-Cl complexes show potent activity against the pathological relevant form of L. infantum amastigote with IC50 in the low micromolar and submicromolar range and five of them exhibit a SI close to 10. The lead-complex 11 displays a very high and selective activity (IC50 = 190 nM, SI = 40.29) and constitutes the best promising gold(I)-based drug of this series.



中文翻译:

中性N-杂环卡宾糖金(I)配合物的合成,表征和抗衰老活性

合成了一系列五个包含N-杂环卡宾(NHCs)的新的单核中性金(I)配合物,并通过光谱法对其进行了全面表征。介绍了四个复合物的X射线结构。这些金(I)配合物以及其他四种先前描述的中性金(I)-NHC配合物在体外针对婴儿利什曼原虫前鞭毛体和轴突性变形虫进行了评估。此外,在鼠巨噬细胞J774A.1上评估了它们的细胞毒性。除了一个复杂的(10),八金(I) - NHC-CL复合物显示对病理相关形式的有效活性婴儿利什曼原虫与IC无鞭毛体50在低微摩尔和亚微摩尔范围内,其中五个具有接近10的SI。铅配合物11显示出非常高的选择性活性(IC 50  = 190 nM,SI = 40.29),是最有希望的金(I)系列药物。

更新日期:2017-10-24
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