Synthesis and anti-HIV activity of 2′-fluorine modified nucleoside phosphonates: Analogs of GS-9148

…, J Douglas, D Grant, O Petrakovsky, V Prasad…

Index: Mackman, Richard L.; Lin, Kuei-Ying; Boojamra, Constantine G.; Hui, Hon; Douglas, Janet; Grant, Deborah; Petrakovsky, Oleg; Prasad, Vidya; Ray, Adrian S.; Cihlar, Tomas Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 3 p. 1116 - 1119

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Citation Number: 23

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.