Chen,JJ (reprint author),Chinese Acad Sci,Kunming Inst Bot,State Key Lab Phytochem & Plant Resources West Ch,Kunming 650201,Peoples R China.
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 mu M. Interestingly, three compounds (22, 28, 29) exhibited excellent activity against the secretion of HBsAg (IC50 = 63.02 mu M, 52.81 mu M, 56.08 mu M), HBeAg (IC50 = 204.80 mu M, 173.51 mu M, 70.39 mu M), along with HBV DNA replication (IC50 = 24.55 mu M, 5.69 mu M, 8.23 mu M) with lower cytotoxicity. The structure-activity relationships (SARs) of these caudatin analogs were also discussed.