| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1376052 | Bioorganic & Medicinal Chemistry Letters | 2007 | 5 Pages |
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 = 2.1 μM, and the most favorable resistance profile against HIV-1 variants with K65R, M184V or multiple thymidine analog mutations in RT.
Graphical abstractA series of ribose and nucleobase modified nucleoside phosphonates have been synthesized and their potency toward wild-type HIV reverse transcriptase (RT) and several mutant strains of RT evaluated.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Richard L. Mackman, 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,