Acridine-decorated cyclometallated gold(iii) complexes: synthesis and anti-tumour investigations

Dalton Trans. 2018 Oct 2;47(38):13523-13534. doi: 10.1039/c8dt02507j.

Abstract

(C^N) and (C^N^C) cyclometalated Au(iii) represent a highly promising class of potential anticancer agents. We report here the synthesis of seven new cyclometalated Au(iii) complexes with five of them bearing an acridine moiety attached via (N^O) or (N^N) chelates, acyclic amino carbenes (AAC) and N-heterocyclic carbenes (NHC). The antiproliferative properties of the different complexes were evaluated in vitro on a panel of cancer cells including leukaemia, lung and breast cancer cells. We observed a trend between the cytotoxicity and the intracellular gold uptake of some representative compounds of the series. Some of the acridine-decorated complexes were demonstrated to interact with ds-DNA using FRET-melting techniques.

MeSH terms

  • Acridines / chemistry*
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / metabolism
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Chemistry Techniques, Synthetic
  • DNA / metabolism
  • Drug Screening Assays, Antitumor
  • Glutathione / metabolism
  • Humans
  • Models, Molecular
  • Molecular Conformation
  • Organogold Compounds / chemical synthesis*
  • Organogold Compounds / chemistry
  • Organogold Compounds / metabolism
  • Organogold Compounds / pharmacology*

Substances

  • Acridines
  • Antineoplastic Agents
  • Organogold Compounds
  • DNA
  • Glutathione