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Bioorg Med Chem Lett. 2004 Apr 5;14(7):1669-72.

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

Author information

1
Department of Bioorganic Medicinal Chemistry, Faculty of Medical and Pharmaceutical Sciences, Kumamoto University, Kumamoto 862-0973, Japan.

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.

PMID:
15026047
DOI:
10.1016/j.bmcl.2004.01.060
[Indexed for MEDLINE]

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