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Scalable Synthesis and Biological Evaluation of 3'-Deoxy-3',4'-didehydronucleoside Triphosphates
Journal article   Peer reviewed

Scalable Synthesis and Biological Evaluation of 3'-Deoxy-3',4'-didehydronucleoside Triphosphates

James M Wood, Dan G Torres, Roselis A Landaeta Aponte, Sandesh Deshpande, Alice M McSweeney, Rinu Shrestha, Andrew Reddy, Gary B Evans, Steven C Almo, Tyler L Grove, …
Journal of organic chemistry, Vol.91(19), pp.6744-6750
04/05/2026
Handle:
https://hdl.handle.net/10523/50879

Abstract

3'-Deoxy-3',4'-didehydronucleoside triphosphates (ddhNTPs) are antiviral metabolites produced by viperin and viperin-like enzymes, all of which are members of the radical SAM superfamily of enzymes. To date, synthetic access to ddhUTP, ddhGTP, and ddhATP has remained limited. We report a scalable synthesis of the complete ddhN nucleoside family using Bobbitt's salt-mediated oxidation of nucleoside orthoformates, including a chromatography-free route to ddhC on a gram scale. This methodology enabled the first synthesis and evaluation of ddhUTP, ddhGTP, and ddhATP as inhibitors of RNA-dependent RNA polymerases, with ddhATP confirmed to act as an obligate chain terminator through primer extension assays.

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