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Comparative in vitro evaluation of N-heterocyclic carbene gold(I) complexes of the benzimidazolylidene type

Gold(I) complexes with a 1,3-diethylbenzimidazol-2-ylidene N-heterocyclic carbene (NHC) ligand of the type NHC-Au-L (L = -Cl, -NHC, or -PPh3) were comparatively evaluated as thioredoxin reductase (TrxR) inhibitors and antimitochondrial anticancer agents. Different effects were noted in various bioch...

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Main Authors: Rubbiani, Riccardo (Author) , Can, Suzan (Author) , Kitanovic, Igor (Author) , Alborzinia, Hamed (Author) , Stefanopoulou, Maria (Author) , Kokoschka, Malte (Author) , Mönchgesang, Susann (Author) , Sheldrick, William S. (Author) , Wölfl, Stefan (Author) , Ott, Ingo (Author)
Format: Article (Journal)
Language:English
Published: 17 November 2011
In: Journal of medicinal chemistry
Year: 2011, Volume: 54, Issue: 24, Pages: 8646-8657
ISSN:1520-4804
DOI:10.1021/jm201220n
Online Access:Verlag, lizenzpflichtig, Volltext: https://doi.org/10.1021/jm201220n
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Author Notes:Riccardo Rubbiani, Suzan Can, Igor Kitanovic, Hamed Alborzinia, Maria Stefanopoulou, Malte Kokoschka, Susann Mönchgesang, William S. Sheldrick, Stefan Wölfl, and Ingo Ott
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Summary:Gold(I) complexes with a 1,3-diethylbenzimidazol-2-ylidene N-heterocyclic carbene (NHC) ligand of the type NHC-Au-L (L = -Cl, -NHC, or -PPh3) were comparatively evaluated as thioredoxin reductase (TrxR) inhibitors and antimitochondrial anticancer agents. Different effects were noted in various biochemical assays (e.g., inhibition of TrxR, cellular and mitochondrial uptake, or effects on mitochondrial membrane potential), and this was related to properties of the complexes such as bond dissociation energies and overall charge. Remarkable antiproliferative effects, a strong induction of apoptosis, and enhancement of reactive oxygen species (ROS) formation as well as other effects on tumor cell metabolism confirmed the promising potential of the complexes as novel anticancer chemotherapeutics.
Item Description:Gesehen am 21.09.2022
Physical Description:Online Resource
ISSN:1520-4804
DOI:10.1021/jm201220n

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