Congratulations to our Ph.D. student Alberto Gobbo for his scientific publication entitled “Ruthenium (II)–Tris-pyrazolylmethane Complexes Inhibit Cancer Cell Growth by Disrupting Mitochondrial Calcium Homeostasis” in the Journal of Medicinal Chemistry. Studies on the medicinal potential of ruthenium complexes containing a tridentate tris(1-pyrazolyl)methane ligand are almost absent in the literature. A straightforward route to access a family of novel, robust and water-soluble cationic ruthenium(II)–tpm complexes was developed. One key ligand modulates both the amphiphilic character and the strength of the ruthenium–chloride bond, which may be implicated in the activation mechanism.
The antiproliferative activity was determined using a panel of human cancer cell lines and a noncancerous one, evidencing promising potency and significant selectivity toward cancer cells. The potency of the leading Ru–tpm complexes was bolstered by the results obtained with the 3D spheroids formed from cancer cells. Most notably, data provide convincing evidence that the mechanism of biological action is mediated by the inhibiting of mitochondrial calcium intake.
The work has been accepted and it can be found at https://pubs.acs.org/doi/full/10.1021/acs.jmedchem.2c00722
