Biscarbene gold(i) complexes

Structure-activity-relationships regarding antibacterial effects, cytotoxicity, TrxR inhibition and cellular bioavailability

verfasst von

Claudia Schmidt, Bianka Karge, Rainer Misgeld, Aram Prokop, Mark Brönstrup, Ingo Ott

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.

Externe Organisation(en)

Technische Universität Braunschweig
Universität zu Köln
Deutsches Zentrum für Infektionsforschung (DZIF)

Typ

Artikel

Journal

MEDCHEMCOMM

Band

8

Seiten

1681-1689

Anzahl der Seiten

9

ISSN

2040-2503

Publikationsdatum

06.2017

Publikationsstatus

Veröffentlicht

Peer-reviewed

Ja

ASJC Scopus Sachgebiete

Biochemie, Molekularmedizin, Pharmakologie, Pharmazeutische Wissenschaften, Wirkstoffforschung, Organische Chemie

Ziele für nachhaltige Entwicklung

SDG 3 – Gute Gesundheit und Wohlergehen

Elektronische Version(en)

https://doi.org/10.1039/c7md00269f (Zugang: Geschlossen)
https://europepmc.org/article/PMC/6072206 (Zugang: Offen)