Issue 8, 2017
From the journal:

MedChemComm

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

Claudia Schmidt, ORCID logo a   Bianka Karge,b   Rainer Misgeld,c   Aram Prokop,c   Mark Brönstrup ORCID logo b  and  Ingo Ott ORCID logo *a  

* Corresponding authors

a Institute of Medicinal and Pharmaceutical Chemistry, Technische Universität Braunschweig, Beethovenstr. 55, 38106 Braunschweig, Germany
E-mail: ingo.ott@tu-bs.de

b Department of Chemical Biology, Helmholtz Centre for Infection Research and German Centre for Infection Research (DZIF), Inhoffenstr. 7, 38124 Braunschweig, Germany

c Department of Pediatric Oncology, Children's Hospital Cologne, Amsterdamer Strasse 59, 50735 Cologne, Germany

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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Article information

DOI
https://doi.org/10.1039/C7MD00269F
Article type
Research Article
Submitted
25 May 2017
Accepted
20 Jun 2017
First published
27 Jun 2017

Med. Chem. Commun., 2017,8, 1681-1689

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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, 8, 1681 DOI: 10.1039/C7MD00269F

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