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Ruthenium(II) Polypyridyl Complexes Containing Simple Dioxo Ligands: a Structure‐Activity Relationship Study Shows the Importance of the Charge

Title	Ruthenium(II) Polypyridyl Complexes Containing Simple Dioxo Ligands: a Structure‐Activity Relationship Study Shows the Importance of the Charge
Authors	Dr. Albert Gandioso, Dr. Alessio Vidal, Dr. Pierre Burckel, Prof. Dr. Gilles Gasser, Prof. Dr. Enzo Alessio
Magazine	Chembiochem
Date	08/26/2022
DOI	10.1002/cbic.202200398
Introduction	Cancer remains a significant global health challenge, with platinum-based treatments such as cisplatin commonly used but often accompanied by severe side effects. Recent studies suggest ruthenium complexes as promising alternatives, particularly Ru(II) polypyridyl complexes, which have demonstrated enhanced anticancer properties. This study investigates two series of such complexes, focusing on their structure-activity relationships. The complexes, characterised as [Ru(L1)2(O^O)]Cln, where L1 represents either 4,7-diphenyl-1,10-phenantroline (DIP) or 1,10-phenanthroline (phen), and O^O denotes oxalate, malonate, or acetylacetonate ligands, were evaluated for their efficacy. Results indicate that the cationic complex [Ru(DIP)2(η2-acac)]Cl exhibits anticancer activity with IC50 values significantly lower than those of cisplatin. Localization studies revealed its primary accumulation in mitochondria, underscoring the critical role of combining positive charge with lipophilic ligands for therapeutic effectiveness.
Quote	Albert Gandioso, Alessio Vidal and Pierre Burckel et al. Ruthenium(II) Polypyridyl Complexes Containing Simple Dioxo Ligands: a Structure-Activity Relationship Study Shows the Importance of the Charge. Chembiochem. 2022. Vol. 23(19). DOI: 10.1002/cbic.202200398

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