title: Phosphonylmethoxyalkyl derivatives of purine as inhibitors of human hepatitis B virus DNA synthesis.
abstract: A selected number of antiviral compounds which have been previously shown to inhibit the replication of DNA viruses or retroviruses were examined for their inhibitory effects on human hepatitis B virus (HBV) DNA synthesis. The assay system was based on the use of a human hepatoblastoma cell line (HB611) that continuously synthesizes HBV DNA. The following phosphonylmethoxyalkyl-purine derivatives were found to inhibit HBV DNA synthesis: 9-(2-phosphonyl-methoxyethyl)-2',6'-diaminopurine (PMEDAP), (S)-9-(3-hydroxy-2-phosphonylmethoxypropyl)adenine (HPMPA) and 9-(2-phosphonylmethoxyethyl)adenine (PMEA). PMEDAP, HPMPA and PMEA not only inhibit HBV DNA synthesis in HB611 cells but also duck hepatitis B virus (DHBV) DNA and core antigen synthesis in primary duck hepatocytes.
authors.affiliation: Department of Bacteriology, Fukushima Medical College, Japan.
authors.forename: T
authors.initials: T
authors.lastname: Yokota
authors.forename: S
authors.initials: S
authors.lastname: Mochizuki
authors.forename: K
authors.initials: K
authors.lastname: Konno
authors.forename: S
authors.initials: S
authors.lastname: Mori
authors.forename: S
authors.initials: S
authors.lastname: Shigeta
authors.forename: E
authors.initials: E
authors.lastname: De Clercq
mesh_terms: D000225:Adenine / Q000031:analogs & derivatives* / Q000494:pharmacology; D000998:Antiviral Agents / Q000494:pharmacology*; D004261:DNA Replication / Q000187:drug effects*; D004279:DNA, Viral / Q000187:drug effects*; D006515:Hepatitis B virus / Q000187:drug effects* / Q000235:genetics; D006801:Humans; D063065:Organophosphonates; D009943:Organophosphorus Compounds / Q000494:pharmacology; D014407:Tumor Cells, Cultured
chemical_list: D000998:Antiviral Agents; D004279:DNA, Viral; D063065:Organophosphonates; D009943:Organophosphorus Compounds; C059499:9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine; C053001:adefovir; C050127:9-(S)-(3-hydroxy-2-(phosphonomethoxy)propyl)adenine; D000225:Adenine