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Synthesis and anti-HIV activity of 2'-fluorine modified nucleoside phosphonates: analogs of GS-9148 |
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| Authors: | Mackman Richard L Lin Kuei-Ying Boojamra Constantine G Hui Hon Douglas Janet Grant Deborah Petrakovsky Oleg Prasad Vidya Ray Adrian S Cihlar Tomas |
| Institution: | Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA. rmackman@gilead.com |
| 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. |
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