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Synthesis of N-Aryl- and N-alkyl-Substituted Imidazolium Silver Complexes: Cytotoxic Screening by Using Human Cell Lines Modelling Acute Myeloid Leukaemia.
ChemMedChem ( IF 3.4 ) Pub Date : 2020-06-17 , DOI: 10.1002/cmdc.202000138
Eirin Alme 1 , Karl Wilhelm Törnroos 1 , Bjørn Tore Gjertsen 2, 3 , Hans-René Bjørsvik 1
Affiliation  

A series of N‐aryl‐ and N‐alkyl substituted imidazoles has been synthesised and complexed with Ag+ to obtain silver‐NHC complexes of the form [Ag(NHC)2]X. These silver‐NHC complexes were tested in vitro against the human cell lines HL‐60 and MOLM‐13, which both model acute myeloid leukaemia (AML). A substantial difference in cytotoxicity was revealed varying in the range 13–4 μM and 22–9 μM for HL‐60 and MOLM‐13, respectively. Furthermore, this study revealed that when an alkyl group is installed on the imidazole scaffold, its position substantially influences the cytotoxicity of the corresponding silver NHC complex.

中文翻译:

N-芳基和N-烷基取代的咪唑银配合物的合成:通过使用人类细胞系建模急性髓细胞白血病的细胞毒性筛选。

合成了一系列的N-芳基和N-烷基取代的咪唑并与Ag +络合,以获得[Ag(NHC)2 ] X形式的银-NHC络合物。这些银-NHC复合物在体外针对人类细胞系HL-60和MOLM-13进行了测试,它们均模拟急性髓细胞白血病(AML)。HL-60和MOLM-13的细胞毒性差异显着,分别在13–4μM和22–9μM之间。此外,这项研究表明,当在咪唑支架上安装烷基时,其位置会实质上影响相应的NHC银配合物的细胞毒性。
更新日期:2020-08-21
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