Tuning the anticancer activity of maltol-derived ruthenium complexes by derivatization of the 3-hydroxy-4-pyrone moiety

Organometallic ruthenium(II)-arene complexes coordinated to maltol-derived ligands were prepared and their anticancer activity against human tumor cell lines was studied. In addition, their hydrolysis behavior and reaction with 5′-GMP was tested and compared to the parent compound chlorido[2-methyl-3-(oxo-κO)-pyran-4(1H)-onato-κO4](η6-p-cymene)ruthenium(II) (Ru-maltol). Improved stability and in vitro anticancer activity at maintained GMP binding capability were observed, in comparison to the Ru-maltol complex.

Graphical abstractOrganometallic ruthenium(II) complexes based on maltol-derived ligands were synthesized and their hydrolysis behavior, reaction to the DNA model 5′-GMP, and anticancer activity against human tumor cell lines was tested. Promising anticancer activity was observed, with the lipophilicity of the compounds appearing to be the determining parameter.Figure optionsDownload full-size imageDownload as PowerPoint slide