Metal complexes of retinoid derivatives with antiproliferative activity: Synthesis, characterization and DNA interaction studies

9-cis-Retinal thiosemicarbazone and its Co(III), Ni(II) and Cu(II) complexes are synthesized and characterized. Central Co(III) atom is in an octahedral environment while Ni(II) and Cu(II) atoms are in a square planar environment. DNA binding constants and spectroscopic data show an intercalative behavior for the nickel complex; an external binding mode is envisaged for the ligand and its copper complex. No DNA interaction can be hypothesized for the cobalt complex. The free ligand and its Ni(II) and Cu(II) complexes have a good lipophilic degree for an efficient uptake by the cells. The metal complexes exhibit a proliferation inhibition action against cell line U937 at micromolar concentration. Cu(II) complex also induces apoptosis, while Ni(II) complex has a strong interaction with CT-DNA.

The syntheses and characterization of 9-cis-retinal thiosemicarbazone Hret and its Co(III), Ni(II) and Cu(II) complexes are reported. The metal complexes exhibit a proliferation inhibition action against human tumor cell line U937 at micromolar concentration. Cu(II) complex also induces apoptosis.Figure optionsDownload as PowerPoint slide