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

  • Bioorg Med Chem Lett. 2004 Apr 5;14(7):1669-72. doi: 10.1016/j.bmcl.2004.01.060.
Mohamed Abdel-Aziz  1 ,  Kazuya Matsuda ,  Masami Otsuka ,  Masaru Uyeda ,  Tadashi Okawara ,  Keitarou Suzuki
Affiliations
  • 1. Department of Bioorganic Medicinal Chemistry, Faculty of Medical and Pharmaceutical Sciences, Kumamoto University, Kumamoto 862-0973, Japan.
PMID: 15026047 DOI: 10.1016/j.bmcl.2004.01.060
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.