SYNTHESIS AND INHIBITORY PROPERTIES OF IMINES CONTAINING MONOTERPENOID AND ADAMANTANE FRAGMENTS AGAINST DNA REPAIR ENZYME TYROSYL-DNA PHOSPHODIESTERASE 1 (Tdp1)

被引：5

作者：

Zakharenko, A. L. ^{[1
]}

Mozhaitsev, E. S. ^{[2
]}

Suslov, E. V. ^{[2
]}

Korchagina, D. V. ^{[2
]}

Volcho, K. P. ^{[2
,3
]}

Salakhutdinov, N. F. ^{[2
,3
]}

Lavrik, O. I. ^{[1
,3
]}

机构：

[1] Russian Acad Sci, Siberian Branch, Inst Chem Biol & Fundamental Med, 8 Prosp Acad Lavrenteva, Novosibirsk 630090, Russia

[2] Russian Acad Sci, Siberian Branch, NN Vorozhtsov Novosibirsk Inst Organ Chem, 9 Prosp Acad Lavrenteva, Novosibirsk 630090, Russia

[3] Novosibirsk State Univ, 2 Pirogova St, Novosibirsk 630090, Russia

来源：

CHEMISTRY OF NATURAL COMPOUNDS | 2018年 / 54卷 / 04期

基金：

俄罗斯科学基金会;

关键词：

adamantane; monoterpene; tyrosyl-DNA phosphodiesterase 1; DNA repair inhibitor; Schiff base; BIOLOGICAL EVALUATION; IDENTIFICATION; CAMPTOTHECIN; MOIETIES; TARGET; TOP1;

D O I：

10.1007/s10600-018-2443-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Six imines including four new ones were synthesized via the reaction of monoterpenoid aldehydes with aminoadamantanes. The inhibitory activities of the synthesized compounds against purified human recombinant DNA repair enzyme tyrosyl-DNA phosphodiesterase 1 (Tdp1) fell in the range IC50 = 5.5-7.1 mu M.

引用

页码：672 / 676

页数：5

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