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

Authors :
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
Source :
Bioorganic & Medicinal Chemistry Letters. Dec2007, Vol. 17 Issue 24, p6785-6789. 5p.
Publication Year :
2007

Abstract

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 EC50 =2.1μM, and the most favorable resistance profile against HIV-1 variants with K65R, M184V or multiple thymidine analog mutations in RT. [Copyright &y& Elsevier]

Details

Language :
English
ISSN :
0960894X
Volume :
17
Issue :
24
Database :
Academic Search Index
Journal :
Bioorganic & Medicinal Chemistry Letters
Publication Type :
Academic Journal
Accession number :
27445211
Full Text :
https://doi.org/10.1016/j.bmcl.2007.10.038