New ruthenium(III) complexes with 3-(Benzothiazol-2-yliminomethyl)-phenol (HL) ligand have been synthesized and characterized with the aid of elemental analysis, IR, electronic, and electron paramagnetic resonance spectroscopic techniques. The binding mode of the ligand and complexes with DNA and their ability to bind DNA have been investigated by UV-vis absorption titration. In addition, the ligand and complexes have been subjected to antioxidant activity tests which showed that HL and its ruthenium(III) complexes possess significant scavenging effect against DPPH and OH radicals. Cytotoxic activities of the ligand and ruthenium(III) complexes showed that the ruthenium(III) complexes exhibited more effective cytotoxic activity against HeLa and MCF-7 cells than the corresponding ligand.