Antiviral Activity of 5’-O-Carbonate 2’,3’-Dideoxy-3’-Thiacytidine Prodrugs Against Hepatitis B Virus in HEPG2 2.2.215 Cells.

GAGEY, DOLORES; RAVETTI, SOLEDAD; CASTRO, ELIANA F.; GUALDESI, MARÍA S.; BRIÑÓN, MARGARITA C.; CAMPOS, RODOLFO H.; CAVALLARO, LUCÍA V.

ELSEVIER SCIENCE BV

Lugar: Amsterdam; Año: 2010 vol. 36 p. 566 - 566

he antiviral activities of lamivudine (3TC; 2,3-dideoxy-3-thiacytidine) and six 5-O-carbonates of 3TC were determined by inhibition of hepatitis B virus (HBV) replication in HepG2 2.2.15 cells. HBV DNA in cell supernatants was quantified by real-time polymerase chain reaction (PCR). The results showed that 3TC-Etha was six times more active than 3TC and that 3TC-Buta, 3TC-Hexa and 3TC-Octa were approximately three times more active than 3TC. In contrast, 3TC-Penta and 3TC-Metha showed anti-HBV activity similar to that of the parent compound 3TC. In conclusion, 5-O-carbonates of 3TC appear to be promising candidates as anti-HBV compounds. This modification could optimise the use of 3TC, a well-tolerated, effective and inexpensive drug, in monotherapy or combined therapy for chronic HBV infections as well as human immunodeficiency virus (HIV)/HBV co-infections.