2. Academic Validation
  3. Aryl nucleoside H-phosphonates. Part 16: synthesis and anti-HIV-1 activity of di-aryl nucleoside phosphotriesters

Aryl nucleoside H-phosphonates. Part 16: synthesis and anti-HIV-1 activity of di-aryl nucleoside phosphotriesters

  • Bioorg Med Chem. 2009 May 1;17(9):3489-98. doi: 10.1016/j.bmc.2009.02.033.
Joanna Romanowska 1,  Agnieszka Szymańska-Michalak,  Jerzy Boryski,  Jacek Stawiński,  Adam Kraszewski,  Roberta Loddo,  Giuseppina Sanna,  Gabriella Collu,  Barbara Secci,  Paolo La Colla
Affiliations

Affiliation

  • 1 Institute of Bioorganic Chemistry, Polish Academy of Sciences, Poznań, Poland.
PMID: 19282192 DOI: 10.1016/j.bmc.2009.02.033
Abstract

Di-aryl nucleoside phosphotriesters have been explored as a new type of pronucleotides for the purpose of anti-HIV-1 therapy and efficient synthetic protocols, based on H-phosphonate chemistry, have been developed for the preparation of this class of compounds. It was found that anti-HIV-1 activity of the phosphotriesters bearing an Antiviral nucleoside moiety (AZT, ddA) and also ddU was due, at least partially, to intracellular conversion into the corresponding nucleoside 5'-monophosphates, and their efficiency correlated well with the pK(a) values of the aryloxy groups present.

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