The synthesis, lipophilicity and cytotoxic effects of new ruthenium(II) arene complexes with chromone derivatives

• Novel arene ruthenium (II) complexes have been synthesized.
• The lipophilicity of synthesized complexes has been determined by shake-flask method.
• The cytotoxicity has been evaluated in vitro in patient derived melanoma cultures.
• The relationship between cytotoxicity and logP values has been determined.

A series of arene ruthenium(II) complexes with the general formula [(η6 − arene)Ru(L)X2] (where arene = p-cymene, benzene, hexamethylbenzene or mesitylene, L = aminoflavone or aminochromone derivatives and X = Cl, I) were synthesized and characterized by elemental analysis, MS, IR and 1H NMR spectroscopy. The stability of the selected complexes was assessed by UV–Vis spectroscopy in 24-hour period. The lipophilicity of the synthesized complexes was determined by the shake-flask method, and their cytotoxicity evaluated in vitro on patient-derived melanoma populations. The most active complexes against melanoma cells contain 7-aminoflavone and 6-aminoflavone as a ligand. The relationship between the cytotoxicity of all the obtained compounds and their logP values was determined and briefly analyzed with two different patterns observed.

The ruthenium(II) arene complexes with the formula [(η6-arene)Ru(L)X2] (where arene = p-cymene, benzene, hexamethylbenzene or mesitylene, L = aminoflavone or aminochromone derivatives and X = Cl, I) have been synthesized. The lipophilic properties and cytotoxic effects of novel complexes have been assayed in order to find structure activity relationship.Figure optionsDownload as PowerPoint slide