4.4 Article

Gold(I) NHC-based homo- and heterobimetallic complexes: synthesis, characterization and evaluation as potential anticancer agents

期刊

JOURNAL OF BIOLOGICAL INORGANIC CHEMISTRY
卷 20, 期 6, 页码 1005-1020

出版社

SPRINGER
DOI: 10.1007/s00775-015-1283-1

关键词

N-heterocyclic carbene; Bimetallic complex; Gold complex; Anticancer drug; Thioredoxin reductase

资金

  1. Centre National de la Recherche Scientifique (ICMUB) [UMR CNRS 6302]
  2. CNRS
  3. Universite de Bourgogne
  4. Conseil Regional de Bourgogne through the 3MIM integrated project (Marquage de Molecules par les Metaux pour l'Imagerie Medicale)
  5. PARI SSTIC
  6. COST Action [TD1004]
  7. University of Groningen
  8. Ministero dell'Istruzione, Universita e Ricerca (MIUR) (Italy) [PRIN 20107Z8XBW]
  9. University of Padova (Italy) [CPDA130272]
  10. Consorzio Interuniversitario di Ricerca in Chimica dei Metalli nei Sistemi Biologici (CIRCSMB)

向作者/读者索取更多资源

While N-heterocyclic carbenes (NHC) are ubiquitous ligands in catalysis for organic or industrial syntheses, their potential to form transition metal complexes for medicinal applications has still to be exploited. Within this frame, we synthesized new homo- and heterobimetallic complexes based on the Au(I)-NHC scaffold. The compounds were synthesized via a microwave-assisted method developed in our laboratories using Au(I)-NHC complexes carrying a pentafluorophenol ester moiety and another Au(I) phosphane complex or a bipyridine ligand bearing a pendant amine function. Thus, we developed two different methods to prepare homo- and heterobimetallic complexes (Au(I)/Au(I) or Au(I)/Cu(II), Au(I)/Ru(II), respectively). All the compounds were fully characterized by several spectroscopic techniques including far infrared, and were tested for their antiproliferative effects in a series of human cancer cells. They showed moderate anticancer properties. Their toxic effects were also studied ex vivo using the precision-cut tissue slices (PCTS) technique and initial results concerning their reactivity with the seleno-enzyme thioredoxin reductase were obtained.

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