Resumen: 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. Idioma: Inglés DOI: 10.1515/pac-2018-0901 Año: 2018 Publicado en: PURE AND APPLIED CHEMISTRY 91, 2 (2018), 247 – 269 ISSN: 0033-4545 Factor impacto JCR: 2.35 (2018) Categ. JCR: CHEMISTRY, MULTIDISCIPLINARY rank: 82 / 172 = 0.477 (2018) - Q2 - T2 Factor impacto SCIMAGO: 1.24 - Chemistry (miscellaneous) (Q1) - Chemical Engineering (miscellaneous) (Q1)