Thirty-nine caudatin analogs were designed and synthesized. Their anti-hepatitis B virus (HBV) activities were
evaluated in vitro. Among them, twenty-three compounds showed much better anti-HBV activity than caudatin, and
eleven compounds significantly inhibited the HBV DNA replication with IC50 values < 10 μM. Interestingly, three compounds
(22, 28, 29) exhibited excellent activity against the secretion of HBsAg (IC50 = 63.02 μM, 52.81 μM, 56.08 μM),
HBeAg (IC50 = 204.80 μM, 173.51 μM, 70.39 μM), along with HBV DNA replication (IC50 = 24.55 μM, 5.69 μM, 8.23 μM) with lower cytotoxicity. The structure-activity relationships (SARs) of these caudatin analogs were also discussed.
Keywords: Anti-HBV activity, Caudatin analogs, Hepatitis B e Antigen (HBeAg), Hepatitis B Surface Antigen (HBsAg),
HBV DNA replication, Structure-activity relationships(SARs), Synthesis.
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