| Literature DB >> 30108879 |
Claudia Schmidt1, Bianka Karge2, Rainer Misgeld3, Aram Prokop3, Mark Brönstrup2, Ingo Ott1.
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.Entities:
Year: 2017 PMID: 30108879 PMCID: PMC6072206 DOI: 10.1039/c7md00269f
Source DB: PubMed Journal: Medchemcomm ISSN: 2040-2503 Impact factor: 3.597