Synthesis, characterization, DNA binding and anticancer activities of the imidazolidine-functionalized (NHC)Ru(II) complexes

Here, we present a study on the synthesis and biological properties of the ruthenium complexes having naphthyl substituted NHC ligands, which are of great importance for drug development studies. For this purpose, in our study, imidazolidine-functionalized Ru(II)NHC complexes containing naphthyl substitute group were synthesized and in vitro anticancer activity as well as DNA binding properties using agarose gel electrophoresis and ethidium bromide fluorescence quenching assay methods were determined in order to understand the biological activities. The Ru(II)NHC complexes were prepared from naphthyl-substituted Ag(I)NHC complexes and [RuCl2(p-cymene)](2) via the transmetallation method. These new complexes were characterized by using H-1 NMR, C-13 NMR, FTIR spectroscopic method and elemental analysis techniques. Consequently, complex 1d showed the highest anticancer activity in terms of IC30 and IC50 values against HepG2 cell line as 23.9 and 32.84 mu M, respectively. Moreover, depending on the data obtained from agarose gel electrophoresis and fluorescence spectrophotometry techniques, 1b had the highest DNA binding property, which means that 1b behaved binding DNA in the cell as an intercalative manner rather than disrupting the integrity of cell membrane like 1d (C) 2021 Elsevier B.V. All rights reserved.

Automated summary

In this study, ruthenium complexes with naphthyl substituted NHC ligands were synthesized and evaluated for their in vitro anticancer activity and DNA binding properties. The results revealed that complex 1d exhibited the highest anticancer activity against HepG2 cell line, while complex 1b showed the highest DNA binding property, indicating their potential biomedical applications.