Design, Synthesis and Biological Evaluation of Caudatin Analogs as Potent Hepatitis B Virus Inhibitors
Wang, Li-Jun1; Chen, Hao1,2; Ma, Yun-Bao1; Huang, Xiao-Yan1; Geng, Chang-An1; Zhang, Xue-Mei1; Chen, Ji-Jun1; Chen,JJ (reprint author),Chinese Acad Sci,Kunming Inst Bot,State Key Lab Phytochem & Plant Resources West Ch,Kunming 650201,Peoples R China.
2015
发表期刊MEDICINAL CHEMISTRY
卷号11期号:2页码:165-179
摘要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.
关键词Anti-hbv Activity Caudatin Analogs Hepatitis b e Antigen (Hbeag) Hepatitis b Surface Antigen (Hbsag) Hbv Dna Replication Structure-activity Relationships(Sars) Synthesis
资助信息National Natural Science Foundation of China for Distinguished Young Scholars [81025023]
收录类别SCI
语种英语
引用统计
文献类型期刊论文
条目标识符http://ir.kib.ac.cn/handle/151853/20611
专题植物化学与西部植物资源持续利用国家重点实验室
通讯作者Chen,JJ (reprint author),Chinese Acad Sci,Kunming Inst Bot,State Key Lab Phytochem & Plant Resources West Ch,Kunming 650201,Peoples R China.
作者单位1.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Peoples R China
2.Chinese Acad Sci, Grad Univ, Beijing 100049, Peoples R China
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Wang, Li-Jun,Chen, Hao,Ma, Yun-Bao,et al. Design, Synthesis and Biological Evaluation of Caudatin Analogs as Potent Hepatitis B Virus Inhibitors[J]. MEDICINAL CHEMISTRY,2015,11(2):165-179.
APA Wang, Li-Jun.,Chen, Hao.,Ma, Yun-Bao.,Huang, Xiao-Yan.,Geng, Chang-An.,...&Chen,JJ .(2015).Design, Synthesis and Biological Evaluation of Caudatin Analogs as Potent Hepatitis B Virus Inhibitors.MEDICINAL CHEMISTRY,11(2),165-179.
MLA Wang, Li-Jun,et al."Design, Synthesis and Biological Evaluation of Caudatin Analogs as Potent Hepatitis B Virus Inhibitors".MEDICINAL CHEMISTRY 11.2(2015):165-179.
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