4.3 Review

Anticancer properties of gold complexes with biologically relevant ligands

Journal

PURE AND APPLIED CHEMISTRY
Volume 91, Issue 2, Pages 247-269

Publisher

WALTER DE GRUYTER GMBH
DOI: 10.1515/pac-2018-0901

Keywords

amino acids; antitumor compounds; Distinguished Women in Chemistry and Chemical Engineering; DNA-base derivatives; gold complexes; peptides

Funding

  1. Ministerio de Economia y Competitividad [MINECO/FEDER CTQ2016-75816-C2-1-P, CTQ2017-88091-P]
  2. Gobierno de Aragon-Fondo Social Europeo

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The present review highlights our findings in the field of antitumor gold complexes bearing biologically relevant molecules, such as DNA-bases, amino acids or peptide derivatives. The results show that very active complexes are achieved with this sort of ligands in several cancer cells. In these compounds the gold center is bonded to these biological molecules mainly through a sulfur atom belonging to a cysteine moiety or to a thionicotinic moiety as result of the functionalization of the biological compounds, and additionally phosphines or N-heterocyclic carbenes are present as ancillary ligands. These robust compounds are stable in the biological media and can be transported to their targets without previous deactivation. The presence of these scaffolds represents a good approach to obtain complexes with improved biologically activity, better transport and biodistribution to cancer cells. Thioredoxin reductase (TrxR) has been shown as the main target for these complexes and in some cases, DNA interactions has been also observed.

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