Inhibition of mammalian topoisomerase I by 1-nitro-9-aminoacridines. Dependence on thiol activation

被引：5

作者：

Ciesielska, E ^{[1
]}

Pastwa, E ^{[1
]}

Szmigiero, L ^{[1
]}

机构：

[1] Med Univ Lodz, Inst Physiol & Biochem, Dept Gen Chem, PL-90131 Lodz, Poland

来源：

ACTA BIOCHIMICA POLONICA | 1997年 / 44卷 / 04期

关键词：

1-nitroacridines; nitracrine; topoisomerase I;

D O I：

10.18388/abp.1997_4381

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The cytotoxic activity, susceptibility to thiol activation and ability of eight 1-nitroacridine derivatives to stabilize the topoisomerase I-DNA cleavable complex, were compared. Among the acridines tested three compounds exhibited high ability to stabilize the cleavable complex. This ability was correlated with susceptibility to thiol activation as well as with cytotoxic activity. Our results suggest that 1-nitroacridine-DNA adducts interfering with topoisomerase I action may contribute to the lethal effects of some 1-nitroacridine derivatives.

引用

页码：775 / 780

页数：6

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