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

…, J Sire, J Neyts, J Balzarini, B Canard, K Alvarez

Index: Barral, Karine; Priet, Stephane; Sire, Josephine; Neyts, Johan; Balzarini, Jan; Canard, Bruno; Alvarez, Karine Journal of Medicinal Chemistry, 2006 , vol. 49, # 26 p. 7799 - 7806

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Citation Number: 11

Abstract

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 α-boranophosphonates 8 and 12 exhibited no significant in vitro activity ...