Literature DB >> 18029175

Synthesis, anti-HIV activity, and resistance profiles of ribose modified nucleoside phosphonates.

Richard L Mackman1, Constantine G Boojamra, Vidya Prasad, Lijun Zhang, Kuei-Ying Lin, Oleg Petrakovsky, Darius Babusis, James Chen, Janet Douglas, Deborah Grant, Hon C Hui, Choung U Kim, David Y Markevitch, Jennifer Vela, Adrian Ray, Tomas Cihlar.   

Abstract

A series of nucleoside phosphonate reverse transcriptase (RT) inhibitors have been synthesized and their anti-HIV activity and resistance profiles evaluated. The most potent analog [5-(6-amino-purin-9-yl)-2,5-dihydro-furan-2-yloxymethyl]-phosphonic acid (d4AP) demonstrated a HIV EC(50)=2.1 microM, and the most favorable resistance profile against HIV-1 variants with K65R, M184V or multiple thymidine analog mutations in RT.

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Year:  2007        PMID: 18029175     DOI: 10.1016/j.bmcl.2007.10.038

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

Review 1.  Synthesis of nucleoside phosphate and phosphonate prodrugs.

Authors:  Ugo Pradere; Ethel C Garnier-Amblard; Steven J Coats; Franck Amblard; Raymond F Schinazi
Journal:  Chem Rev       Date:  2014-08-21       Impact factor: 60.622

2.  Pyrrolidine nucleotide analogs with a tunable conformation.

Authors:  Lenka Poštová Slavětínská; Dominik Rejman; Radek Pohl
Journal:  Beilstein J Org Chem       Date:  2014-08-22       Impact factor: 2.883

  2 in total

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