A series of new mononuclear cationic or neutral gold(I) complexes containing quinoline functionalized N-heterocyclic carbene(s) (NHC(s)) were synthesized and fully characterized by spectroscopic methods. The X-ray structures of two key compounds are presented. Proligands and their corresponding gold(I) complexes together with previously described silver(I) and gold(I) bis(NHC-quinoline) and gold(I) bis(NHC-methylbipyridine) complexes were evaluated in vitro towards Leishmania infantum. In parallel, the in vitro cytotoxicity of these molecules was assessed on the murine macrophages J774A.1. All gold(I) compounds show potent antileishmanial activity against L. infantum promastigotes and three of them are also efficient against L. infantum intracellular amastigotes. Structure-activity and toxicity relationships enables to evidence a lead-compound (6) displaying both a high activity and a good selectivity index.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/j.ejmech.2015.02.046 | DOI Listing |
Eur J Med Chem
December 2024
Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization, School of Medicine, Nanjing University of Chinese Medicine, Nanjing, 210023, PR China. Electronic address:
Overexpression of epidermal growth factor receptor (EGFR) and thioredoxin reductase (TrxR) are commonly associated with an adverse prognosis in hepatocellular carcinoma (HCC). This makes them key targets for the treatment of HCC. Studies have shown that the clinical efficacy of the EGFR tyrosine kinase inhibitor gefitinib alone in treating HCC is limited.
View Article and Find Full Text PDFInorg Chem
December 2024
Contribution from the Department of Chemistry, University of California, Davis, California 95616, United States.
Five new crystalline gold(I) complexes β-Au(μ-dppm)Br·2CHCl (), [Au(μ- dppm)Br]Br·2CHCl (), [Au(μ-dppm)Br](PF) (), [Au(μ-dppm)Cl](BPh)·3CHCl () and [Au(μ-dppm)]Cl(AsF)·2CHCl () (where dppm is bis(diphenylphosphino)methane) have been prepared and structurally characterized by single crystal X-ray diffraction. Colorless β-Au(μ-dppm)Br·2CHCl () has centrosymmetric structure with two three-coordinate gold(I) ions held in close proximity by the dppm ligands. Crystals of [Au(μ- dppm)Br]Br·2CHCl (), [Au(μ-dppm)Br](PF) (), and [Au(μ-dppm)Cl](BPh)·3CHCl () have a cation with an unusual arrangement that binds a two-coordinate gold(I) ion to a three-coordinate gold(I) ion through an aurophilic interaction.
View Article and Find Full Text PDFJ Phys Chem A
December 2024
Facultad de Ciencias, Departamento de Químicas, Universidad de Chile, Casilla 653, Santiago 1025000, Chile.
We present a study of the cooperative nature of the forces dominating the interaction between gold atoms and aryl-aryl stacking. For this purpose, we modeled a series of complexes of the type dpm(AuR) (dpm= bis(phoshino)methane; R = -CH, -CF, -CCl, and -Cl). The models were calculated at the MP2, CCSD(T), and DFT-D3(BJ) (PBE and TPSS) levels of theory.
View Article and Find Full Text PDFDalton Trans
December 2024
Department of Chemistry, University of Kentucky, Lexington, KY 40506, USA.
Rationalizing the impact of oxidation states of Au-based complexes on function require synthetic strategies that allow for conserved molecular formula in Au(I) and their Au(III) counterparts. Oftentimes achieving Au(I) and Au(III) coordination complexes with the same ligand system is challenging due to the reactivity and stability of the starting Au(I) or Au(III) starting materials. Thus, attempts to study the impact of oxidation state on biological function has been elusive.
View Article and Find Full Text PDFDalton Trans
December 2024
Department of Chemistry, Texas A & M University, College Station, Texas 77843, USA.
The templating properties of a diaza-nickel--dithiolate towards triphenylphosphine gold(I), yielding a [Ni(NS)·2Au(PPh)] complex (T. A. Pinder, S.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!