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A gold(I) biscarbene complex with improved activity as a TrxR inhibitor and cytotoxic drug: comparative studies with different gold metallodrugs

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Abstract

Gold complexes with N-heterocyclic carbene (NHC) ligands have been attracting major attention in medicinal inorganic chemistry based on their favorable antiproliferative effects and the structural versatility of the coordinated NHC ligands. Here we present a novel complex of the type (NHC)2Au+, which represents a substantially improved and selective TrxR inhibitor compared to close structural analogues. The complex is highly stable in various solutions over 96 hours, however, comparative cellular uptake studies indicate metabolic transformations inside cells over time. A portfolio of other gold complexes (e.g. Auranofin) has been used as references in key biological assays, showing that the novel (NHC)2Au+ complex exhibits substantially lower protein binding in combination with a strongly enhanced cytotoxic activity.

Graphical abstract: A gold(i) biscarbene complex with improved activity as a TrxR inhibitor and cytotoxic drug: comparative studies with different gold metallodrugs

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Publication details

The article was received on 25 Oct 2018, accepted on 26 Nov 2018 and first published on 26 Nov 2018


Article type: Paper
DOI: 10.1039/C8MT00306H
Citation: Metallomics, 2019, Advance Article

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    A gold(I) biscarbene complex with improved activity as a TrxR inhibitor and cytotoxic drug: comparative studies with different gold metallodrugs

    C. Schmidt, L. Albrecht, S. Balasupramaniam, R. Misgeld, B. Karge, M. Brönstrup, A. Prokop, K. Baumann, S. Reichl and I. Ott, Metallomics, 2019, Advance Article , DOI: 10.1039/C8MT00306H

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