Open AccessInhibition of mammalian topoisomerase I by 1-nitro-9-aminoacridines. Dependence on thiol activation.
Author(s) -
Ewa Ciesielska,
Elżbieta Pastwa,
Leszek Szmigiero
Publication year - 1997
Publication title -
acta biochimica polonica
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.452
H-Index - 78
eISSN - 1734-154X
pISSN - 0001-527X
DOI - 10.18388/abp.1997_4381
Subject(s) - topoisomerase , thiol , chemistry , cytotoxic t cell , dna , adduct , enzyme , stereochemistry , nitro , biochemistry , in vitro , organic chemistry , alkyl
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.