Synthesis and biological activity of 7H-benzo[4,5]indolo[2,3-b]-quinoxaline derivatives

被引：11

作者：

Shibinskaya, Marina O. ^{[1
]}

Karpenko, Alexander S. ^{[1
]}

Lyakhov, Sergey A. ^{[1
,2
]}

Andronati, Sergey A. ^{[1
,2
]}

Zholobak, Nadezhda M. ^{[3
]}

Spivak, Nikolay Ya. ^{[3
]}

Samochina, Natalia A. ^{[4
]}

Shafran, Lev M. ^{[4
]}

Zubritskye, Mykhail Ju. ^{[5
]}

Galat, Valerij F. ^{[5
]}

机构：

[1] NAS Ukraine, AV Bogatsky Physicochem Inst, UA-65080 Odessa, Ukraine

[2] Odessa Natl II Mechnikov Univ, UA-65026 Odessa, Ukraine

[3] NAS Ukraine, DK Zabolotny Inst Microbiol & Virol, UA-03143 Kiev, Ukraine

[4] Ukrainian Sci & Res Inst Med Transport, UA-65039 Odessa, Ukraine

[5] NAS Ukraine, LM Litvinenko Inst Phys Organ Chem & Coal Chem, UA-83114 Donetsk, Ukraine

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2011年 / 46卷 / 02期

关键词：

7H-benzo[4,5]indolo[2,3-b]quinoxaline; Anti-viral activity; Interferon induction; DNA affinity; STACKING INTERACTIONS; ANTIVIRAL ACTIVITY; DNA; AGENTS;

D O I：

10.1016/j.ejmech.2010.11.040

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

New 7-(2-aminoethyl)-7H-benzo[4,5]indolo[2,3-b]quinoxalines (13-20) were synthesized with high yields starting from 3H-benzo[e]indole-1,2-dione. These compounds were screened for the cytotoxicity, anti-viral activity, interferon inducing ability and DNA affinity compared with the corresponding 6-(2-aminoethyl)-6H-indolo[2,3-b]quinoxaline derivatives (1-12). It was shown, that compounds 13-20 bind to DNA stronger (Ig K-a = 6.23-6.87) than compounds 1-12 (Ig K-a = 5.57-5.89). Anti-viral activity is significantly reduced with annulations of benzene ring in Indoloquinoxaline moiety 13-20. (C) 2010 Elsevier Masson SAS. All rights reserved.

引用

页码：794 / 798

页数：5

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