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

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

Volume: 11 Issue: 2

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

Affiliation:

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

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.

Cite this article as:

Wang Li-Jun, Chen Hao, Ma Yun-Bao, Huang Xiao-Yan, Geng Chang-An, Zhang Xue-Mei and Chen Ji-Jun, Design, Synthesis and Biological Evaluation of Caudatin Analogs as Potent Hepatitis B Virus Inhibitors, Medicinal Chemistry 2015; 11 (2) . https://dx.doi.org/10.2174/1573406410666140902111326