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. 2017 Jun 15;27(12):2800-2802.
doi: 10.1016/j.bmcl.2017.04.069. Epub 2017 Apr 22.

Flex-nucleoside analogues - Novel therapeutics against filoviruses

Mary K Yates  1 , Mithun R Raje  1 , Payel Chatterjee  2 , Christina F Spiropoulou  2 , Sina Bavari  3 , Mike Flint  2 , Veronica Soloveva  3 , Katherine L Seley-Radtke  4
Affiliations

Flex-nucleoside analogues - Novel therapeutics against filoviruses

Mary K Yates et al. Bioorg Med Chem Lett. .

Abstract

Fleximers, a novel type of flexible nucleoside that have garnered attention due to their unprecedented activity against human coronaviruses, have now exhibited highly promising levels of activity against filoviruses. The Flex-nucleoside was the most potent against recombinant Ebola virus in Huh7 cells with an EC50=2μM, while the McGuigan prodrug was most active against Sudan virus-infected HeLa cells with an EC50 of 7μM.

Keywords: Antiviral; Ebola; Filovirus; Fleximers; Nucleoside.

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Figures

None
Graphical abstract
Fig. 1
Fig. 1
Nucleoside based inhibitors with reported anti-Ebola activity.
Fig. 2
Fig. 2
Structure of Acyclovir and the target flexible nucleoside analogues.
Scheme 1
Scheme 1
Reagents and conditions: (a) Na2 SO3, 30% EtOH, 120 °C, 84%; (b) Ac2O, NEt3,DMAP, 97%; (c) Pd2dba3 CHCl3,5 or 6, Cul, CsF, DMF, 50 °C, 20%.
Scheme 2
Scheme 2
(a) tBuMgCl, THF, 69%.
See this image and copyright information in PMC

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