Novel Synthetic Azaacridine Analogues as Topoisomerase 1 Inhibitors

被引：15

作者：

Luan, Xudong ^{[1
,2
]}

Gao, Chunmei ^{[1
]}

Sun, Qinsheng ^{[1
]}

Tan, Chunyan ^{[1
]}

Liu, Hongxia ^{[1
]}

Jin, Yibao ^{[1
,2
]}

Jiang, Yuyang ^{[1
,2
,3
]}

机构：

[1] Tsinghua Univ, Grad Sch Shenzhen, Guangdong Prov Key Lab Chem Biol, Shenzhen 518055, Peoples R China

[2] Tsinghua Univ, Dept Chem, Beijing 100084, Peoples R China

[3] Tsinghua Univ, Sch Med, Beijing 100084, Peoples R China

来源：

CHEMISTRY LETTERS | 2011年 / 40卷 / 07期

关键词：

DNA; CHEMOTHERAPY; DERIVATIVES;

D O I：

10.1246/cl.2011.728

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Novel azaacridine analogues were synthesized and their antiproliferative activities against K562 and HepG-2 cell lines were evaluated, among which compound 5a was found to display good cytotoxicity. UV-visible spectral absorbance measurements showed that 5a can bind with calf thymus DNA (ct DNA). A relaxation assay indicated that 5a inhibits topoisomerase 1 activity.

引用

收藏

页码：728 / 729

页数：2

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