Naphtho[2,3-f]indole-5,10-dione aminoalkyl derivatives:: A new class of topoisomerase I inhibitors

被引：3

作者：

Dezhenkova, L. G. ^{[2
]}

Susova, O. Yu. ^{[1
]}

Shchekotikhin, A. E. ^{[2
]}

Preobrazhenskaya, M. N. ^{[2
]}

Shtil, A. A. ^{[1
]}

机构：

[1] Russian Acad Med Sci, Inst Carcinogenesis, NN Blokhin Natl Canc Res Ctr, Moscow 109801, Russia

[2] Russian Acad Med Sci, GF Gauze Inst Search New Antibiot, Moscow 109801, Russia

来源：

BULLETIN OF EXPERIMENTAL BIOLOGY AND MEDICINE | 2008年 / 145卷 / 03期

基金：

俄罗斯基础研究基金会;

关键词：

naphthoindole diones; topoisomerase I; cytotoxicity; tumor cells;

D O I：

10.1007/s10517-008-0084-8

中图分类号：

R-3 [医学研究方法]; R3 [基础医学];

学科分类号：

1001 ;

摘要：

Naphtho[2,3-f]indole-5,10-dione aminoalkyl derivatives in cytotoxic concentrations inhibit topoisomerase I, which is an important factor of antitumor activity of compounds of this chemical class. The degree of topoisomerase I inhibition with naphtho[2,3-f]indole-5,10-dione derivatives depends on the structure and position of active (aminoalkyl) groups. The mechanism of topoisomerase I inhibition with aminoalkylnaphtho[2,3-f]indole-5,10-diones differs from specific blocking of the catalytic activity of the enzyme and depends on interactions of these compounds with DNA.

引用

页码：334 / 337

页数：4

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