Design, synthesis, and molecular hybrids of caudatin and cinnamic acids as novel anti-hepatitis B virus agents
文献类型：期刊论文
| 作者 | 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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| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
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| 出版日期 | 2012-08-01 |
| 卷号 | 54页码:352-365 |
| 关键词 | Synthesis Molecular hybrids Caudatin derivatives Anti-hepatitis B virus Unique mechanisms |
| ISSN号 | 0223-5234 |
| 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 |
| 英文摘要 | 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. |
| 类目[WOS] | Chemistry, Medicinal |
| 研究领域[WOS] | Pharmacology & Pharmacy |
| 关键词[WOS] | GENE-EXPRESSION ; PREGENOMIC PROMOTER ; ANTIVIRAL ACTIVITY ; BINDING-PROTEIN ; IN-VITRO ; X-GENE ; DERIVATIVES ; HBV ; ENHANCER ; INHIBITORS |
| 收录类别 | SCI ; IC |
| 资助信息 | National Natural Science Foundation of China for Distinguished Young Scholars [81025023] |
| 语种 | 英语 |
| WOS记录号 | WOS:000307920600037 |
| 公开日期 | 2012-11-30 |
| 源URL | [http://ir.kib.ac.cn/handle/151853/15720]  |
| 专题 | 昆明植物研究所_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. |
入库方式： OAI收割
来源：昆明植物研究所
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