o-, m-, p-Phenylenediamines having 2, 3, 4-trihydroxy, 3, 4 dihydroxy, and 4-hydroxybenzoyl moieties were prepared and their inhibitory activities were measured against topoisomerase I and II. More hydroxy groups on two aromatic rings increased the activities. Bis (trihydroxybenzoyl)-o-phenylenediamide showed IC50= 0.90 and 0.09 μM against topoisomerase I and II, respectively. Compounds with hydroxy groups protected by acetyl ...