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

Abstract

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.

• Authors: R A Heijtink, J Kruining, G A de Wilde, J Balzarini, E de Clercq, S W Schalm
• Journal: Antimicrobial agents and chemotherapy (Antimicrob Agents Chemother) Vol. 38 Issue 9 Pg. 2180-2 (Sep 1994) ISSN: 0066-4804 [Print] United States
• PMID: 7811041 (Publication Type: Journal Article)

Chemical References

• 9-(2-phosphonylmethoxypropyl)-2,6-diaminopurine
• Antiviral Agents
• Nucleosides
• Organophosphonates
• Organophosphorus Compounds
• Purines
• Cytosine
• Adenine

Topics

• 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