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

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• 作者：Marina O. Shibinskaya ; Alex ; er S. Karpenko ; Sergey A. Lyakhov ; Sergey A. Andronati ; Nadezhda M. Zholobak ; Nikolay Ya. Spivak ; Natalia A. Samochina ; Lev M. Shafran ; Mykhail Ju. Zubritsky ; Valerij F. Galat
• 关键词：7H-benzo[4 ; 5]indolo[2 ; 3-b]quinoxaline ; Anti-viral activity ; Interferon induction ; DNA affinity
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2011
• 出版时间：February 2011
• 年：2011
• 卷：46
• 期：2
• 页码：794-798
• 全文大小：215 K

文摘

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 (lg К_a = 6.23–6.87) than compounds 1–12 (lg К_a = 5.57–5.89). Anti-viral activity is significantly reduced with annulations of benzene ring in Indoloquinoxaline moiety 13–20.