Literature DB >> 30108879

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

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


  35 in total

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2.  Inhibition Mechanism of Urease by Au(III) Compounds Unveiled by X-ray Diffraction Analysis.

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3.  Crystal structures of the gold NHC complex bis-(4-bromo-1,3-di-ethyl-imidazol-2-yl-idene)gold(I) iodide and its 1:1 adduct with trans-bis-(4-bromo-1,3-diethyl-imidazol-2-yl-idene)di-iodido-gold(III) iodide.

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5.  Improved Antiproliferative Activity and Fluorescence of a Dinuclear Gold(I) Bisimidazolylidene Complex via Anthracene-Modification.

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7.  Antibacterial Thiamine inspired silver (I) and gold (I) N-heterocyclic carbene compounds.

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8.  Internal and External Influences on Stability and Ligand Exchange Reactions in Bromido[3-ethyl-4-aryl-5-(2-methoxypyridin-5-yl)-1-propyl-1,3-dihydro-2H-imidazol-2-ylidene]gold(I) Complexes.

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9.  NHC-gold compounds mediate immune suppression through induction of AHR-TGFβ1 signalling in vitro and in scurfy mice.

Authors:  Xinlai Cheng; Stefanie Haeberle; Iart Luca Shytaj; Rodrigo A Gama-Brambila; Jannick Theobald; Shahrouz Ghafoory; Jessica Wölker; Uttara Basu; Claudia Schmidt; Annika Timm; Katerina Taškova; Andrea S Bauer; Jörg Hoheisel; Nikolaos Tsopoulidis; Oliver T Fackler; Andrea Savarino; Miguel A Andrade-Navarro; Ingo Ott; Marina Lusic; Eva N Hadaschik; Stefan Wölfl
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