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Design, Synthesis and Biological Evaluation of Caudatin Analogs as Potent Hepatitis B Virus Inhibitors

[ Vol. 11 , Issue. 2 ]


Li-Jun Wang, Hao Chen, Yun-Bao Ma, Xiao-Yan Huang, Chang-An Geng, Xue-Mei Zhang and Ji-Jun Chen   Pages 165 - 179 ( 15 )


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.


Anti-HBV activity, Caudatin analogs, Hepatitis B e Antigen (HBeAg), Hepatitis B Surface Antigen (HBsAg), HBV DNA replication, Structure-activity relationships(SARs), Synthesis.


State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, PR China.

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