Oxiranylmethyloxy or thiiranylmethyloxy-azaxanthones and -acridone analogues as potential topoisomerase I inhibitors

被引：29

作者：

Cho, Hee-Ju ^{[2
]}

Jung, Mi-Ja ^{[1
]}

Kwon, Youngjoo ^{[1
]}

Na, Younghwa ^{[2
]}

机构：

[1] Ewha Womans Univ, Coll Pharm, Seoul 120750, South Korea

[2] Catholic Univ Daegu, Coll Pharm, Gyongsan 712702, Gyeongbuk, South Korea

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 23期

关键词：

Azaxanthone; Acridone; Topoisomerase I inhibitor; Anticancer agents; AGENTS;

D O I：

10.1016/j.bmcl.2009.09.091

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A total of seven new oxyranylmethyloxy or thiiranylmethyloxy group substituted 5-azaxanthones and -acridones analogues were synthesized and tested for their biological activities for cancer cell lines and topoisomerases. Among the compounds, compound 5, 3-thiiranylmethyloxy-1-hydroxy-5-azaxanthone, showed effective topoisomerase I inhibitory activity, 50% and 27% inhibition ratio at 100 and 20 mu M, respectively. This result is the first finding of the function of 5-azaxanthone compounds for topoisomerase I inhibition and can provide a novel skeleton for the anticancer drug development process. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：6766 / 6769

页数：4

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