Biscarbene gold(I) complexes: structure–activity-relationships regarding antibacterial effects, cytotoxicity, TrxR inhibition and cellular bioavailability,RSC Medicinal Chemistry

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Biscarbene gold(I) complexes: structure–activity-relationships regarding antibacterial effects, cytotoxicity, TrxR inhibition and cellular bioavailability
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2017-06-27 00:00:00 , DOI: 10.1039/c7md00269f
Claudia Schmidt _{1,

2,

3,

4} , Bianka Karge _{4,

5,

6,

7} , Rainer Misgeld _{4,

8,

9,

10} , Aram Prokop _{4,

8,

9,

10} , Mark Brönstrup _{4,

5,

6,

7} , Ingo Ott _{1,

2,

3,

4}

Affiliation

A series of gold(I) complexes with two N-heterocyclic carbene ligands (biscarbene gold complexes) were prepared and evaluated for their effects against cancer cells and pathogenic bacteria. Proliferation inhibition was observed in cancer cells and in Gram-positive bacteria, whereas Gram-negative bacteria were less sensitive towards the compounds. The protein binding and cellular uptake were quantified and the combined results indicated a strong correlation between cellular bioavailability and antiproliferative effects. The biscarbene gold complexes inhibited bacterial and mammalian TrxRs with low to moderate potency. However, based on the obtained structure–activity-relationships and the high cellular accumulation levels, TrxR inhibition can be considered as a relevant contributor to the cellular pharmacology of biscarbene gold(I) complexes.

中文翻译：

双卡宾金（I）配合物：关于抗菌作用，细胞毒性，TrxR抑制和细胞生物利用度的结构-活性-关系

一系列的金（我制备了具有两个N-杂环卡宾配体的复合物（双卡宾金配合物），并评估了它们对癌细胞和病原菌的作用。在癌细胞和革兰氏阳性细菌中观察到了增殖抑制作用，而革兰氏阴性细菌对该化合物的敏感性较低。定量蛋白质结合和细胞摄取，合并的结果表明细胞生物利用度和抗增殖作用之间有很强的相关性。双卡宾金络合物以低至中等的效力抑制细菌和哺乳动物的TrxR。然而，基于获得的结构-活性关系和高细胞蓄积水平，TrxR抑制可被认为是双卡宾金的细胞药理学的相关贡献（I）复合体。

更新日期：2017-08-16

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