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

E Ciesielska; E Pastwa; L Szmigiero

doi:10.18388/abp.1997_4381

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

E Ciesielska Department of General Chemistry, Institute of Physiology and Biochemistry, Medical University in Lódź, Poland.;
E Pastwa
L Szmigiero

DOI: https://doi.org/10.18388/abp.1997_4381

Abstract

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.

Published

1997-12-31

Issue

Vol. 44 No. 4 (1997)

Section

Articles

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