| 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
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| 通讯作者 | Chen, JJ (reprint author), Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources W China, 132 Lanhei Rd, Heilongtan 650201, Kunming, Peoples R China.,chenjj@mail.kib.ac.cn |
| 2012-08-01 | |
| 发表期刊 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
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| ISSN | 0223-5234 |
| 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 |
| DOI | 10.1016/j.ejmech.2012.05.012 |
| 收录类别 | SCI ; IC |
| 语种 | 英语 |
| WOS记录号 | WOS:000307920600037 |
| 引用统计 | |
| 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 |
| 推荐引用方式 GB/T 7714 | 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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