Synthesis, structure-activity relationships and biological evaluation of caudatin derivatives as novel anti-hepatitis B virus agents
Wang, Li-Jun1,2; Geng, Chang-An1; Ma, Yun-Bao1; Huang, Xiao-Yan1; Luo, Jie1; Chen, Hao1,2; Guo, Rui-Hua1,2; Zhang, Xue-Mei1; Chen, Ji-Jun1
2012-05-01
发表期刊BIOORGANIC & MEDICINAL CHEMISTRY
ISSN0968-0896
卷号20期号:9页码:2877-2888
摘要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. Among the tested compounds, six compounds (2e-2h, 2l, 2r) exhibited significantly inhibitory activity against HBV DNA replication with IC50 values in the range of 2.82-7.48 mu M. Interestingly, two compounds (2e, 2f) had potent activity inhibiting not only the secretion of HBsAg (IC50 = 18.68 mu M, 21.71 mu M), HBeAg (IC50 = 13.16 mu M, 33.73 mu M), but also HBV DNA replication (IC50 = 7.48 mu M, 3.63 mu M). The structure-activity relationships (SARs) of caudatin derivatives had been discussed, which were useful for caudatin derivatives to be explored and developed as novel anti-HBV agents. (C) 2012 Elsevier Ltd. All rights reserved.
关键词Synthesis Caudatin Derivatives Anti-hbv Activity Structure-activity Relationships
资助信息National Natural Science Foundation of China for Distinguished Young Scholars[81025023]
学科领域Biochemistry & Molecular Biology ; Chemistry, Medicinal ; Chemistry, Organic
DOI10.1016/j.bmc.2012.03.023
收录类别SCI
语种英语
WOS研究方向Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
WOS类目Biochemistry & Molecular Biology ; Chemistry, Medicinal ; Chemistry, Organic
WOS记录号WOS:000303002100013
引用统计
被引频次:15[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.kib.ac.cn/handle/151853/10441
专题植物化学与西部植物资源持续利用国家重点实验室
作者单位1.Chinese Acad Sci, State Key Lab Phytochem & Plant Resources W China, Kunming Inst Bot, Kunming 650201, Peoples R China
2.Chinese Acad Sci, Grad Univ, Beijing 100049, Peoples R China
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Wang, Li-Jun,Geng, Chang-An,Ma, Yun-Bao,et al. Synthesis, structure-activity relationships and biological evaluation of caudatin derivatives as novel anti-hepatitis B virus agents[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2012,20(9):2877-2888.
APA Wang, Li-Jun.,Geng, Chang-An.,Ma, Yun-Bao.,Huang, Xiao-Yan.,Luo, Jie.,...&Chen, Ji-Jun.(2012).Synthesis, structure-activity relationships and biological evaluation of caudatin derivatives as novel anti-hepatitis B virus agents.BIOORGANIC & MEDICINAL CHEMISTRY,20(9),2877-2888.
MLA Wang, Li-Jun,et al."Synthesis, structure-activity relationships and biological evaluation of caudatin derivatives as novel anti-hepatitis B virus agents".BIOORGANIC & MEDICINAL CHEMISTRY 20.9(2012):2877-2888.
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