Inhibitory effects of acyclic nucleoside phosphonates on human hepatitis B virus and duck hepatitis B virus infections in tissue culture.

The inhibitory effects of the 9-(2-phosphonylmethoxyethyl)adenine-related compounds (S)-9-(3-hydroxy-2-phosphonylmethoxypropyl)-adenine, (S)-9-(3-fluoro-2-phosphonylmethoxypropyl)adenine, (R)-9-(2-phosphonylmethoxypropyl)adenine, (R)-9-(2-phosphonylmethoxypropyl)-2,6-diaminopurine, and (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine on human hepatitis B virus replication in the human hepatoma cell line HepG2 2.2.15 and duck hepatitis B virus infection in primary duck hepatocytes were investigated. (R)-9-(2-phosphonylmethoxypropyl-2,6-diaminopurine had the lowest 50% inhibitory concentrations against hepatitis B virus and duck hepatitis B virus, 0.22 and 0.06 microM, respectively, i.e., two- to fivefold lower concentrations than required for (R)-9-(2-phosphonylmethoxypropyl)adenine and 9-(2-phosphonylmethoxyethyl)adenine. All compounds were not toxic in vitro at a concentration of 100 microM.
AuthorsR A Heijtink, J Kruining, G A de Wilde, J Balzarini, E de Clercq, S W Schalm
JournalAntimicrobial agents and chemotherapy (Antimicrob Agents Chemother) Vol. 38 Issue 9 Pg. 2180-2 (Sep 1994) ISSN: 0066-4804 [Print] UNITED STATES
PMID7811041 (Publication Type: Journal Article)
Chemical References
  • 9-(2-phosphonylmethoxypropyl)-2,6-diaminopurine
  • Antiviral Agents
  • Nucleosides
  • Organophosphonates
  • Organophosphorus Compounds
  • Purines
  • Cytosine
  • Adenine
  • Adenine (analogs & derivatives, pharmacology)
  • Animals
  • Antiviral Agents (pharmacology)
  • Carcinoma, Hepatocellular (virology)
  • Cytosine (analogs & derivatives)
  • Ducks
  • Hepatitis B Virus, Duck (drug effects)
  • Hepatitis B virus (drug effects)
  • Humans
  • Liver (cytology, virology)
  • Liver Neoplasms (virology)
  • Nucleosides (pharmacology)
  • Organophosphonates (pharmacology)
  • Organophosphorus Compounds (pharmacology)
  • Purines (pharmacology)
  • Tumor Cells, Cultured

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