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

Modified purine analogs of nucleoside phosphonate GS-9148 (2′F-d4AP) were synthesized and their anti-HIV activity evaluated. 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 eva...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2008-02, Vol.18 (3), p.1116-1119
Hauptverfasser:	Mackman, Richard L., Lin, Kuei-Ying, Boojamra, Constantine G., Hui, Hon, Douglas, Janet, Grant, Deborah, Petrakovsky, Oleg, Prasad, Vidya, Ray, Adrian S., Cihlar, Tomas
Format:	Artikel
Sprache:	eng
Schlagworte:	Anti-HIV Agents - chemical synthesis Anti-HIV Agents - chemistry Anti-HIV Agents - pharmacology Antibiotics. Antiinfectious agents. Antiparasitic agents Antiviral Antiviral agents Biological and medical sciences Fluorine - chemistry Guanosine - analogs & derivatives Guanosine - chemical synthesis Guanosine - chemistry Guanosine - pharmacology HIV Human immunodeficiency virus Humans Medical sciences Molecular Structure Nucleosides - chemical synthesis Nucleosides - chemistry Nucleosides - pharmacology Organophosphonates - chemical synthesis Organophosphonates - chemistry Organophosphonates - pharmacology Pharmacology. Drug treatments Phosphonate Reverse Transcriptase Inhibitors - chemical synthesis Reverse Transcriptase Inhibitors - chemistry Reverse Transcriptase Inhibitors - pharmacology Structure-Activity Relationship Zidovudine - pharmacology
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Zusammenfassung:	Modified purine analogs of nucleoside phosphonate GS-9148 (2′F-d4AP) were synthesized and their anti-HIV activity evaluated. 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.
ISSN:	0960-894X 0968-0896 1464-3405 1464-3391
DOI:	10.1016/j.bmcl.2007.11.126