Arene Ruthenium Complexes with Ethacrynic Acid-Modified Ligands: Synthesis, Characterization and Antiproliferative Activity

Ethacrynic acid is a broad acting glutathione transferase inhibitor, and its incorporation within suitable metal complexes results in enhancement of the anticancer activity.1 A series of pyridine- and phosphine-based ligands functionalized with ethacrynic acid were synthesized and coordinated to ruthenium(II)-arene complexes. All the compounds (ligands and complexes) were fully characterized by different analytical and spectroscopic techniques and, in some cases, by single-crystal X-ray diffraction. The in vitro anticancer activity of the compounds was studied towards two different tumour cell lines, the compounds displaying moderate antiproliferative activity.2 The interactions with two well-known model proteins were analysed through ESI MS spectrometry and the resulting metallodrug–protein adducts identified.