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

被引：25

作者：

Abdel-Aziz, M

Matsuda, K

Otsuka, M

Uyeda, M

Okawara, T

Suzuki, K ^{[1
]}

机构：

[1] Kumamoto Univ, Fac Med & Pharmaceut Sci, Dept Pharmaceut Microbiol, Kumamoto 8620973, Japan

[2] Kumamoto Univ, Fac Med & Pharmaceut Sci, Dept Bioorgan Med Chem, Kumamoto 8620973, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 07期

关键词：

polyhydroxybenzoyl amide; topoisomerase inhibitor; structure-activity relationship;

D O I：

10.1016/j.bmcl.2004.01.060

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 muM against topoisomerase I and 11, 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. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：1669 / 1672

页数：4

共 27 条

[21] Isoaurostatin, a novel topoisomerase inhibitor produced by Thermomonospora alba [J].