Adding diversity to ruthenium(II)–arene anticancer (RAPTA) compounds via click chemistry: The influence of hydrophobic chains

The application of click chemistry to develop libraries of organometallic ruthenium–arene complexes with potential anticancer properties has been investigated. A series of ruthenium–imidazole–triazole complexes, with hydrophobic tails, were prepared from a common precursor via click chemistry. The tail could be attached to the ligand prior to coordination to the ruthenium complex or following coordination, the former giving the product in superior yield. The complexes were screened for cytotoxicity in tumourigenic and non-tumourigenic cell lines, and while the compounds were only moderately cytotoxic, good selectivity for tumourigenic cells was observed.

Graphical abstractClick chemistry was used to prepare a series of organometallic ruthenium–arene complexes with hydrophobic tails that display high selectivity and moderate anticancer activity in vitro.Figure optionsDownload full-size imageDownload as PowerPoint slideResearch highlights►The application of click chemistry to generate collections of ruthenium-arene compounds. ► Evaluation of the anticancer properties of the compounds in vitro ► Studies into the mode of action of the compounds.