An overview on the anticancer activity of Ru(II)/acylthiourea complexes

[Display omitted] •The chemistry of ruthenium/acylthiourea ligands is reviewed.•The coordination properties of acylthiourea ligands are highlighted.•This review covers anticancer activity, in vitro, of Ru(II)/acylthiourea complexes.•Structure-activity relationships and trends are discussed. This review outlines research on the development of ruthenium complexes containing acylthiourea ligands with potential antitumor activity, which have been leveraged in recent years. Also, this review sheds light on the fact that the coordination of biologically active acylthiourea molecules has been yielding a variety of complexes with superior biological activity to their precursor complexes and free ligands. The structure–activity relationships for several structure scaffolds of ruthenium complexes with different coordination modes of both, N-mono- and disubstituted acylthiourea ligands, are discussed here in relation to in vitro cytotoxic properties and in vivo antitumor activity. Another insight gained from this review is the understanding of the correlation between the nature of the substituents on the amide and thioamide moieties of the acylthiourea ligands, and the cytotoxic activity of their respective complexes. Furthermore, the mode of binding of Ru-acylthiourea complexes to DNA is explored to provide information on whether the biomolecule is a possible primary target of these compounds, and thus, whether it is a justification for the cytotoxic action of the complexes.