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.
|Keywords||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 Neoplasms/virology, Liver/cytology/virology, Nucleosides/*pharmacology, Organophosphorus Compounds/pharmacology, Phosphonic Acids/*pharmacology, Purines/pharmacology, Tumor Cells, Cultured|
Heijtink, R.A., Kruining, J., de Wilde, G.A., Balzarini, J., de Clercq, E., & Schalm, S.W.. (1994). Inhibitory effects of acyclic nucleoside phosphonates on human hepatitis B virus and duck hepatitis B virus infections in tissue culture. Antimicrobial Agents and Chemotherapy. Retrieved from http://hdl.handle.net/1765/8564