Synthesis and anti-HIV activity of 2'-fluorine modified nucleoside phosphonates: analogs of GS-9148

  • Bioorg Med Chem Lett. 2008 Feb 1;18(3):1116-9. doi: 10.1016/j.bmcl.2007.11.126.
Richard L Mackman  1 ,  Kuei-Ying Lin ,  Constantine G Boojamra ,  Hon Hui ,  Janet Douglas ,  Deborah Grant ,  Oleg Petrakovsky ,  Vidya Prasad ,  Adrian S Ray ,  Tomas Cihlar
Affiliations
  • 1. Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA. [email protected]
PMID: 18082402 DOI: 10.1016/j.bmcl.2007.11.126
Abstract

Modified purine analogs of GS-9148 [5-(6-amino-purin-9-yl)-4-fluoro-2,5-dihydro-furan-2-yloxymethyl]-phosphonic acid (2'-Fd4AP) were synthesized and their anti-HIV potency evaluated. The Antiviral activity of Guanosine analog (2'-Fd4GP) was comparable that of to 2'-Fd4AP in MT-2 cells, but selectivity was reduced.