Synthesis, structure-activity relationships and biological evaluation of caudatin derivatives as novel anti-hepatitis B virus agents

A series of caudatin derivatives were synthesized, and their anti-hepatitis B virus (HBV) activity was evaluated in HepG 2.2.15 cells. Most of the 3-O-substituted caudatin derivatives showed effective anti-HBV activity. Two compounds (2e, 2f) had potent activity inhibiting not only the secretion of HBsAg, HBeAg, but also HBV DNA replication. The structure-activity relationships (SARs) of caudatin derivatives had been discussed.