Author: Vakhrusheva, Diana V. ; Charushin, Valery N. ; Pervova, Marina G. ; Eremeeva, Natalya I. ; Belyaev, Danila V. ; Rusinov, Gennady L. ; Khramtsova, Ekaterina E. ; Sadykhov, Gusein A. ; Verbitskiy, Egor V. ; Chupakhin, Oleg N.

AbstractA convenient synthetic protocol to antiviral agent B‐220 and a series of similar indolo[2,3‐b]quinoxaline derivatives has been developed. This synthetic approach is based on Buchwald‐Hartwig cross‐coupling and subsequent annulation by intramolecular oxidative cyclodehydrogenation. For the first time, 6H‐indolo[2,3‐b]quinoxaline amine derivatives were evaluated for antimycobacterial activity. The moderate bacteriostatic effect against Mycobacterium tuberculosis H37Rv was found. A plausible mechanism of antibacterial action was elucidated by the molecular docking.

01 Aug 2017·Bioorganic & Medicinal Chemistry LettersQ4 · MEDICINE

Virtual screening, synthesis and biological evaluation of DNA intercalating antiviral agents

Q4 · MEDICINE

Article

Author: Marina Zenkova ; Rinat Amirkhanov ; Elena Goncharova ; Andrei Krysko ; Kyrylo Klimenko ; Alexandre Varnek ; Dragos Horvath ; Marina Shibinskaya ; Pavel Polishchuk ; Victor Kuz'min ; Igor Levandovskiy ; Sergei Andronati ; Sergey Lyakhov ; Gilles Marcou ; Alexander Karpenko

This paper describes computer-aided design of new anti-viral agents against Vaccinia virus (VACV) potentially acting as nucleic acid intercalators. Earlier obtained experimental data for DNA intercalation affinities and activities against Vesicular stomatitis virus (VSV) have been used to build, respectively, pharmacophore and QSAR models. These models were used for virtual screening of a database of 245 molecules generated around typical scaffolds of known DNA intercalators. This resulted in 12 hits which then were synthesized and tested for antiviral activity against VaV together with 43 compounds earlier studied against VSV. Two compounds displaying high antiviral activity against VaV and low cytotoxicity were selected for further antiviral activity investigations.

01 Feb 2011·European Journal of Medicinal ChemistryQ1 · MEDICINE

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

Q1 · MEDICINE

Article

Author: Nikolay Ya. Spivak ; Lev M. Shafran ; Nadezhda M. Zholobak ; Alexander S. Karpenko ; Marina O. Shibinskaya ; Natalia A. Samochina ; Sergey A. Lyakhov ; Valerij F. Galat ; Sergey A. Andronati ; Mykhail Ju. Zubritsky

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

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Indication	Highest Phase	Country/Location	Organization	Date
Colonic Cancer	Preclinical	China	Xiamen University	-

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