Topoisomerase IIα-IN-2 (compound 5) is a DNA-binding ligands and a potent inhibitor of the topoisomerase TopoIIα. Topoisomerase IIα-IN-2 exhibits high anti-proliferative activity in human cancer cell lines. Topoisomerase IIα-IN-2 arrests the cell cycle of cancer cells in the G2/M phase and significantly induces DNA damage.