132178-47-3Relevant articles and documents
Synthesis, anti-HIV activity, and resistance profiles of ribose modified nucleoside phosphonates
Mackman, Richard L.,Boojamra, Constantine G.,Prasad, Vidya,Zhang, Lijun,Lin, Kuei-Ying,Petrakovsky, Oleg,Babusis, Darius,Chen, James,Douglas, Janet,Grant, Deborah,Hui, Hon C.,Kim, Choung U.,Markevitch, David Y.,Vela, Jennifer,Ray, Adrian,Cihlar, Tomas
, p. 6785 - 6789 (2008/09/18)
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 EC50 = 2.1 μM, and the most favorable resistance profile against HIV-1 variants with K65R, M184V or multiple thymidine analog mutations in RT.