Design, Synthesis and Biological Evaluation of Caudatin Analogs as Potent Hepatitis B Virus Inhibitors
文献类型：期刊论文
| 作者 | Wang, Li-Jun1; Chen, Hao1,2; Ma, Yun-Bao1; Huang, Xiao-Yan1; Geng, Chang-An1 ; Zhang, Xue-Mei1; Chen, Ji-Jun1
|
| 刊名 | MEDICINAL CHEMISTRY
 |
| 出版日期 | 2015 |
| 卷号 | 11期号:2页码:165-179 |
| 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 |
| 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. |
| 英文摘要 | 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. |
| 学科主题 | Chemistry, Medicinal |
| 类目[WOS] | Chemistry, Medicinal |
| 研究领域[WOS] | Pharmacology & Pharmacy |
| 关键词[WOS] | ANTI-HBV ; ACID-DERIVATIVES ; DRUG-RESISTANCE ; AGENTS ; REPLICATION ; ALISOL ; CELLS |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000349331700008 |
| 源URL | [http://ir.kib.ac.cn/handle/151853/20611]  |
| 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 West Ch, Kunming 650201, 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,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, Ji-Jun.(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. |
入库方式： OAI收割
来源：昆明植物研究所
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