Inhibitory effects of selected antiviral compounds on human hepatitis B virus DNA synthesis.
By using an assay system based on a human hepatoblastoma cell line (HB611) that continuously synthesizes hepatitis B virus DNA, the following compounds were found to inhibit hepatitis B virus DNA synthesis at concentrations that were significantly lower than their minimum cytotoxic concentrations: 9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine (PMEDAP), (S)-9-(3-hydroxy-2-phosphonylmethoxypropyl)adenine, 9-(phosphonylmethoxyethyl)adenine, 2',3'-dideoxy-2',3'-didehydrocytidine, and 2',3'-dideoxycytidine. The most potent compound was PMEDAP (50% effective concentration, 0.02 micrograms/ml). The selective index, or ratio of the 50% cytotoxic concentration to 50% effective concentration, of PMEDAP was greater than 750.
Yokota
T
T
Department of Bacteriology, Fukushima Medical College, Fukushima, Japan.
Mochizuki
S
S
Konno
K
K
Mori
S
S
Shigeta
S
S
De Clercq
E
E
D000998:Antiviral Agents / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects; D004261:DNA Replication / Q000187:drug effects; D004279:DNA, Viral / Q000096:biosynthesis*; D015224:Dideoxynucleosides / Q000494:pharmacology; D015611:Hepatitis B Virus, Duck / Q000187:drug effects / Q000378:metabolism*; D013936:Thymidine; D014407:Tumor Cells, Cultured
D000998:Antiviral Agents; D004279:DNA, Viral; D015224:Dideoxynucleosides; D013936:Thymidine