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Feb 2010 European journal of medicinal chemistry

Synthesis and antiviral activity of boranophosphonate isosteres of AZT and d4T monophosphates.


Barral K, Priet S, De Michelis C, Sire J, Neyts J, Balzarini J, Canard B, Alvarez K


We report synthesis, in vitro antiviral activity, and stability studies in biological media of original boranophosphonate isosteres of AZT and d4T monophophates. A convenient route for the synthesis of 3′-Azido-3′-deoxythymidine-5′-boranophosphonate 8 and 2′,3′-Didehydro-3′-dideoxythymidine-5′-boranophosphonate 12 is described. H-phosphinates 7 and 11, and alpha-boranophosphonates 8 and 12 exhibited no significant in vitro activity against HIV-infected cells, neither against a broad panel of viruses, up to 200 microM. The absence of activity of target compounds 8 and 12 can be partially explained by their short half-life in culture medium.

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