Synthesis and anti-HIV activity of GS-9148 (2′-Fd4AP), a novel nucleoside phosphonate HIV reverse transcriptase inhibitor

Compound 4 (2′-Fd4AP) was synthesized and maintained the favorable anti-HIV properties of 2 while demonstrating a marked reduction in mitochondrial toxicity to HepG2 cells. GS-9148 (2′-Fd4AP, 4) has been identified as a nucleoside phosphonate reverse transcriptase (RT) inhibitor with activity agains...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2008-02, Vol.18 (3), p.1120-1123
Hauptverfasser:	Boojamra, Constantine G., Mackman, Richard L., Markevitch, David Y., Prasad, Vidya, Ray, Adrian S., Douglas, Janet, Grant, Deborah, Kim, Choung U., 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 DNA, Mitochondrial - drug effects Fluorine - chemistry Guanosine - analogs & derivatives Guanosine - chemical synthesis Guanosine - chemistry Guanosine - pharmacology HIV HIV Reverse Transcriptase - genetics 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 Resistance Reverse Transcriptase Inhibitors - chemical synthesis Reverse Transcriptase Inhibitors - chemistry Reverse Transcriptase Inhibitors - pharmacology Structure-Activity Relationship Zidovudine - pharmacology
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