Details
| Originalsprache | Englisch |
|---|---|
| Seiten (von - bis) | 1681-1689 |
| Seitenumfang | 9 |
| Fachzeitschrift | MEDCHEMCOMM |
| Jahrgang | 8 |
| Ausgabenummer | 8 |
| Publikationsstatus | Veröffentlicht - Juni 2017 |
| Extern publiziert | Ja |
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.
ASJC Scopus Sachgebiete
- Biochemie, Genetik und Molekularbiologie (insg.)
- Biochemie
- Biochemie, Genetik und Molekularbiologie (insg.)
- Molekularmedizin
- Pharmakologie, Toxikologie und Pharmazie (insg.)
- Pharmakologie
- Pharmakologie, Toxikologie und Pharmazie (insg.)
- Pharmazeutische Wissenschaften
- Pharmakologie, Toxikologie und Pharmazie (insg.)
- Wirkstoffforschung
- Chemie (insg.)
- Organische Chemie
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in: MEDCHEMCOMM, Jahrgang 8, Nr. 8, 06.2017, S. 1681-1689.
Publikation: Beitrag in Fachzeitschrift › Artikel › Forschung › Peer-Review
}
TY - JOUR
T1 - Biscarbene gold(i) complexes
T2 - Structure-activity-relationships regarding antibacterial effects, cytotoxicity, TrxR inhibition and cellular bioavailability
AU - Schmidt, Claudia
AU - Karge, Bianka
AU - Misgeld, Rainer
AU - Prokop, Aram
AU - Brönstrup, Mark
AU - Ott, Ingo
N1 - Funding Information: Financial support from Deutsche Forschungsgemeinschaft (DFG) is gratefully acknowledged (project codes: OT338/12-1 and BR3572/4-1). We thank Dr. Raimo Franke (HZI) for fruitful discussions and his support of this study.
PY - 2017/6
Y1 - 2017/6
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=85027526082&partnerID=8YFLogxK
U2 - 10.1039/c7md00269f
DO - 10.1039/c7md00269f
M3 - Article
AN - SCOPUS:85027526082
VL - 8
SP - 1681
EP - 1689
JO - MEDCHEMCOMM
JF - MEDCHEMCOMM
SN - 2040-2503
IS - 8
ER -