Design, synthesis, and molecular hybrids of caudatin and cinnamic acids as novel anti-hepatitis B virus agents
Wang, Li-Jun1,2; Geng, Chang-An1; Ma, Yun-Bao1; Luo, Jie1; Huang, Xiao-Yan1; Chen, Hao1,2; Zhou, Ning-Jia1,2; Zhang, Xue-Mei1; Chen, Ji-Jun1
2012-08-01
发表期刊EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
ISSN0223-5234
卷号54页码:352-365
摘要Forty-six conjugated derivatives of caudatin with substituted cinnamic acids were synthesized, and their anti-hepatitis B virus (HBV) activity was evaluated in HepG 2.2.15 cells. Most of the derivatives exhibited potent anti-HBV activity, especially inhibiting the HBV DNA replication with the IC50 values from 2.44 to 22.89 mu M. Compound 18 showed significant activity against the secretion of HBsAg, HBeAg, and HBV DNA replication with IC50 values of 5.52, 5.52, 2.44 mu M, respectively, and had good safety (LD50 > 1250 mg/kg) according to the acute toxicity study. Preliminary mechanism investigation suggested that compound 18 exerted antivirus effects via interfering HBV X promoter and enhancer 1 to influence HBV transcriptions. (C) 2012 Elsevier Masson SAS. All rights reserved.
关键词Synthesis Molecular Hybrids Caudatin Derivatives Anti-hepatitis b Virus Unique Mechanisms
资助信息National Natural Science Foundation of China for Distinguished Young Scholars [81025023]
DOI10.1016/j.ejmech.2012.05.012
收录类别SCI ; IC
语种英语
WOS研究方向Pharmacology & Pharmacy
WOS类目Chemistry, Medicinal
WOS记录号WOS:000307920600037
引用统计
被引频次:23[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/151853/15720
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, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources W China, Heilongtan 650201, Kunming, 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. Design, synthesis, and molecular hybrids of caudatin and cinnamic acids as novel anti-hepatitis B virus agents[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2012,54:352-365.
APA Wang, Li-Jun.,Geng, Chang-An.,Ma, Yun-Bao.,Luo, Jie.,Huang, Xiao-Yan.,...&Chen, Ji-Jun.(2012).Design, synthesis, and molecular hybrids of caudatin and cinnamic acids as novel anti-hepatitis B virus agents.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,54,352-365.
MLA Wang, Li-Jun,et al."Design, synthesis, and molecular hybrids of caudatin and cinnamic acids as novel anti-hepatitis B virus agents".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 54(2012):352-365.
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