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

Author(s): Li-Jun Wang, Hao Chen, Yun-Bao Ma, Xiao-Yan Huang, Chang-An Geng, Xue-Mei Zhang, Ji-Jun Chen

Journal Name: Medicinal Chemistry

Volume 11 , Issue 2 , 2015

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Graphical Abstract:


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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Article Details

Year: 2015
Page: [165 - 179]
Pages: 15
DOI: 10.2174/1573406410666140902111326
Price: $65

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