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. 2004 Apr 5;14(7):1669-72.
doi: 10.1016/j.bmcl.2004.01.060.

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

Mohamed Abdel-Aziz  1 , Kazuya Matsuda, Masami Otsuka, Masaru Uyeda, Tadashi Okawara, Keitarou Suzuki
Affiliations

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

Mohamed Abdel-Aziz et al. Bioorg Med Chem Lett. .

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 IC(50)=0.90 and 0.09 microM against topoisomerase I and II, respectively. Compounds with hydroxy groups protected by acetyl moiety still had the activities. Less hydroxy groups decreased their activities. Benzothiazole derivatives also indicated the activities.

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