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

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Abstract

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.

Graphical abstract: Biscarbene gold(i) complexes: structure–activity-relationships regarding antibacterial effects, cytotoxicity, TrxR inhibition and cellular bioavailability

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Publication details

The article was received on 25 May 2017, accepted on 20 Jun 2017 and first published on 27 Jun 2017


Article type: Research Article
DOI: 10.1039/C7MD00269F
Citation: Med. Chem. Commun., 2017, Advance Article
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    Biscarbene gold(I) complexes: structure–activity-relationships regarding antibacterial effects, cytotoxicity, TrxR inhibition and cellular bioavailability

    C. Schmidt, B. Karge, R. Misgeld, A. Prokop, M. Brönstrup and I. Ott, Med. Chem. Commun., 2017, Advance Article , DOI: 10.1039/C7MD00269F

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