Inhibitory activities against topoisomerase I & II by polyhydroxybenzoyl amide derivatives and their structure–activity relationship

M Abdel-Aziz, K Matsuda, M Otsuka, M Uyeda…

Index: Abdel-Aziz, Mohamed; Matsuda, Kazuya; Otsuka, Masami; Uyeda, Masaru; Okawara, Tadashi; Suzuki, Keitarou Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 7 p. 1669 - 1672

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Citation Number: 14

Abstract

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 ...