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Solving the challenging synthesis of highly cytotoxic silver complexes bearing sterically hindered NHC ligands with mechanochemistry.
Dalton Transactions ( IF 4 ) Pub Date : 2020-08-24 , DOI: 10.1039/d0dt00410c
Audrey Beillard 1 , François Quintin 1 , Jérémie Gatignol 2 , Pascal Retailleau 3 , Jean-Luc Renaud 2 , Sylvain Gaillard 2 , Thomas-Xavier Métro 1 , Frédéric Lamaty 1 , Xavier Bantreil 1
Affiliation  

The use of ball-mills enabled the straightforward synthesis of a variety of silver(I) complexes featuring challenging NHC ligands. Sterically hindered including electron-poor or with very low solubility imidazolium salts were ground with silver(I) oxide to furnish heteroleptic or homoleptic complexes in high yields and short reaction times. The synthesis of heteroleptic bis-NHC silver(I) complexes was also performed for the first time in a ball mill. The efficiency and rapidity of the mechanochemical approach enabled the generation of a library of unprecedented NHC silver complexes, whose cytotoxicity on the HCT116 colorectal cancer cell line was evaluated providing a rare example of medicinal mechanochemistry. The cationic silver complexes were found to be more potent than the neutral analogues, with IC50 values down to 21 nM and 256 times more potent than cisplatin.

中文翻译:

用机械化学方法解决具有位阻性NHC配体的高细胞毒性银络合物的合成难题。

使用球磨机可以直接合成具有挑战性NHC配体的各种银(I)配合物。包括电子贫乏或溶解度非常低的受阻位咪唑鎓盐与氧化银(I)一起研磨,以高收率和较短的反应时间提供杂配或均配的配合物。杂合双-NHC银的合成(I)复合物也是第一次在球磨机中进行。机械化学方法的效率和快速性使得能够生成空前的NHC银复合物文库,评估了其对HCT116结肠直肠癌细胞系的细胞毒性,为药物机械化学提供了一个罕见的例子。发现阳离子银配合物比中性类似物更有效,IC 50值低至21 nM,且比顺铂强256倍。
更新日期:2020-09-22
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