Biologically active phi X174 DNA is inactivated by the ortho-quinone derivative of the antitumor agent VP 16-213, but not by VP 16-213 itself, VP 16-213 phenoxy radical or aqueous decomposition product(s) of the ortho-quinone. Reduction of the ortho-quinone by cytochrome P-450 reductase and NADPH results in deactivation of the ortho-quinone towards anti-phi X174 DNA activity. However, compared with the parent compound VP 16-213, reduction of the ortho-quinone results in substantial damage towards DNA.