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.

Organometallic 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 as PowerPoint slide