2. Academic Validation
  3. Synthesis, anti-HIV activity, and resistance profiles of ribose modified nucleoside phosphonates

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

  • Bioorg Med Chem Lett. 2007 Dec 15;17(24):6785-9. doi: 10.1016/j.bmcl.2007.10.038.
Richard L Mackman 1,  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
Affiliations

Affiliation

  • 1 Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA. [email protected]
PMID: 18029175 DOI: 10.1016/j.bmcl.2007.10.038
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.

Figures