Isoxazolidinyl polycyclic aromatic hydrocarbons as DNA-intercalating antitumor agents

► Isoxazolidinyl polycyclic aromatic hydrocarbons act as DNA-intercalator agents. ► A fine tuning of these isoxazolidinyl-PAH substrates is relevant to synthesize drugs that could bind DNA specifically to AT or GC nucleobases. ► The most potent of them showed an IC50 of 9 mM upon the human lung cancer (A-549) cell and a binding constant, for the intercalation with calf thymus DNA, of 9.6 × 104 M−1.