Novel ring-expanded nucleoside analogs exhibit potent and selective inhibition of hepatitis B virus replication in cultured human hepatoblastoma cells.
Antiviral Res
; 53(2): 159-64, 2002 Feb.
Article
en En
| MEDLINE
| ID: mdl-11750942
ABSTRACT
Novel ring-expanded nucleoside (REN) analogs (1-3) containing 57 fused ring systems as the heterocyclic base were found to be potent and selective inhibitors of hepatitis B virus (HBV) replication in cultured human hepatoblastoma 2.2.15 cells. The most active compound, 6-amino-4,5-dihydro-8H-1-(beta-D-ribofuranosyl)imidazo[4,5-e][1,3]diazepine-4,8-dione (1), inhibited the synthesis of intracellular HBV replication intermediates and extracellular virion release in 2.2.15 cells with 50% effective concentration (EC50) of 0.604 and 0.131 microM, respectively. All three compounds had no effect on the synthesis of viral ribonucleic acids (RNA) in 2.2.15 cells. These compounds also exhibited low cellular toxicity in stationary and rapidly growing cell systems.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Antivirales
/
Replicación Viral
/
Virus de la Hepatitis B
/
Nucleósidos
Límite:
Humans
Idioma:
En
Revista:
Antiviral Res
Año:
2002
Tipo del documento:
Article
País de afiliación:
Estados Unidos