Usnic Acid Derivatives Are Effective Inhibitors of Tyrosyl-DNA Phosphodiesterase 1

被引:19
|
作者
Zakharenko, A. L. [1 ]
Luzina, O. A. [2 ]
Sokolov, D. N. [2 ]
Zakharova, O. D. [1 ]
Rakhmanova, M. E. [3 ]
Chepanova, A. A. [4 ]
Dyrkheeva, N. S. [1 ]
Lavrik, O. I. [1 ,3 ,4 ]
Salakhutdinov, N. F. [2 ,3 ]
机构
[1] Russian Acad Sci, Siberian Branch, Inst Chem Biol & Fundamental Med, Novosibirsk 630090, Russia
[2] Russian Acad Sci, Siberian Branch, Vorozhtsov Novosibirsk Inst Organ Chem, Novosibirsk 630090, Russia
[3] Novosibirsk State Univ, Novosibirsk 630090, Russia
[4] Altai State Univ, Barnaul 656049, Russia
基金
俄罗斯科学基金会;
关键词
tyrosyl-DNA phosphodiesterase 1; tyrosyl-DNA phosphodiesterase 1 inhibitors; usnic acid; BIOLOGICAL EVALUATION; TDP1; IDENTIFICATION; ASSAY;
D O I
10.1134/S1068162017010125
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 synthesis of (+)-usnic acid derivatives is described. The derivatives contain one or two cyano groups, connected to the acetophenone fragment of dibenzofuran core by linkers of different length and character, or some other modifications. The influence of these compounds on the activity of recombinant human tyrosyl-DNA phosphodiesterase 1 and MCF-7 tumor cells' viability has been estimated. The data indicate a distinct dependence of functional characteristics of the compounds on their structure.
引用
收藏
页码:84 / 90
页数:7
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