2. Academic Validation
  3. Phenoxazine nucleoside derivatives with a multiple activity against RNA and DNA viruses

Phenoxazine nucleoside derivatives with a multiple activity against RNA and DNA viruses

  • Eur J Med Chem. 2021 Aug 5:220:113467. doi: 10.1016/j.ejmech.2021.113467.
Liubov I Kozlovskaya 1,  Viktor P Volok 2,  Anna A Shtro 3,  Yulia V Nikolaeva 3,  Alexey A Chistov 4,  Elena S Matyugina 5,  Evgeny S Belyaev 6,  Artjom V Jegorov 4,  Robert Snoeck 7,  Vladimir A Korshun 4,  Graciela Andrei 7,  Dmitry I Osolodkin 1,  Aydar A Ishmukhametov 1,  Andrey V Aralov 8
Affiliations

Affiliations

  • 1 FSBSI "Chumakov FSC R&D IBP RAS", Moscow, 108819, Russia; Institute of Translational Medicine and Biotechnology, Sechenov Moscow State Medical University, Moscow, 119991, Russia.
  • 2 FSBSI "Chumakov FSC R&D IBP RAS", Moscow, 108819, Russia.
  • 3 Smorodintsev Research Institute of Influenza, Saint-Petersburg, 197376, Russia.
  • 4 Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Moscow, 117997, Russia.
  • 5 Engelhardt Institute of Molecular Biology, Moscow, 119991, Russia.
  • 6 Frumkin Institute of Physical Chemistry and Electrochemistry of the Russian Academy of Science, Moscow, 119071, Russia.
  • 7 Rega Institute for Medical Research, KU Leuven, Leuven, Belgium.
  • 8 Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Moscow, 117997, Russia. Electronic address: Baruh238@mail.ru.
PMID: 33894564 DOI: 10.1016/j.ejmech.2021.113467
Abstract

Emerging and re-emerging viruses periodically cause outbreaks and epidemics all over the world, eventually leading to global events such as the current pandemic of the novel SARS-CoV-2 coronavirus Infection COVID-19. Therefore, an urgent need for novel antivirals is crystal clear. Here we present the synthesis and evaluation of an Antiviral activity of phenoxazine-based nucleoside analogs divided into three groups: (1) 8-alkoxy-substituted, (2) acyclic, and (3) carbocyclic. The Antiviral activity was assessed against a structurally and phylogenetically diverse panel of RNA and DNA viruses from 25 species. Four compounds (11a-c, 12c) inhibited 4 DNA/RNA viruses with EC50 ≤ 20 μM. Toxicity of the compounds for the cell lines used for virus cultivation was negligible in most cases. In addition, previously reported and newly synthesized phenoxazine derivatives were evaluated against SARS-CoV-2, and some of them showed promising inhibition of reproduction with EC50 values in low micromolar range, although accompanied by commensurate cytotoxicity.

Keywords

Antivirals; DNA viruses; Nucleoside analogs; Phenoxazine; RNA viruses; SARS-CoV-2.

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