| Synthesis, structure-activity relationships and biological evaluation of dehydroandrographolide and andrographolide derivatives as novel anti-hepatitis B virus agents | |
Chen, Hao1,2; Ma, Yun-Bao1; Huang, Xiao-Yan1; Geng, Chang-An1 ; Zhao, Yong1,2; Wang, Li-Jun1; Guo, Rui-Hua1; Liang, Wen-Juan1,2; Zhang, Xue-Mei1; Chen, Ji-Jun1
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| 通讯作者 | Chen,JJ (reprint author),Chinese Acad Sci,State Key Lab Phytochem & Plant Resources West C,Kunming Inst Bot,Kunming 650201,Peoples R China. ; chenjj@mail.kib.ac.cn |
| 2014-05-15 | |
| 发表期刊 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
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| ISSN | 0960-894X |
| 卷号 | 24期号:10页码:2353-2359 |
| 摘要 | Dehydroandrographolide and andrographolide, two natural diterpenoids isolated from Andrographis paniculata possessed activity against HBV DNA replication with IC50 values of 22.58 and 54.07 mu M and low SI values of 8.7 and 3.7 in our random assay. Consequently, 48 derivatives of dehydroandrographolide and andrographolide were synthesized and evaluated for their anti-HBV properties to yield a series of active derivatives with lower cytotoxicity, including 14 derivatives against HBsAg secretion, 19 derivatives against HBeAg secretion and 38 derivatives against HBV DNA replication. Interestingly, compound 4e could inhibit not only HBsAg and HBeAg secretions but also HBV DNA replication with SI values of 20.3, 125.0 and 104.9. Furthermore, the most active compound 2c with SI value higher than 165.1 inhibiting HBV DNA replication was revealed with the optimal logP value of 1.78 and logD values. Structureactivity relationships (SARs) of the derivatives were disclosed for guiding the future research toward the discovery of new anti-HBV drugs. (C) 2014 Elsevier Ltd. All rights reserved. |
| 关键词 | Anti-hbv Activity DehydroAndrographolide And Andrographolide Derivatives Structure-activity Relationships Octanol-water Partition Coefficients |
| 学科领域 | Pharmacology & Pharmacy ; Chemistry |
| DOI | 10.1016/j.bmcl.2014.03.060 |
| 收录类别 | SCI ; IC |
| 语种 | 英语 |
| WOS记录号 | WOS:000335517300024 |
| 引用统计 | |
| 文献类型 | 期刊论文 |
| 条目标识符 | http://ir.kib.ac.cn/handle/151853/18112 |
| 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 West C, Kunming Inst Bot, Kunming 650201, Peoples R China 2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China |
| 推荐引用方式 GB/T 7714 | Chen, Hao,Ma, Yun-Bao,Huang, Xiao-Yan,et al. Synthesis, structure-activity relationships and biological evaluation of dehydroandrographolide and andrographolide derivatives as novel anti-hepatitis B virus agents[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2014,24(10):2353-2359. |
| APA | Chen, Hao.,Ma, Yun-Bao.,Huang, Xiao-Yan.,Geng, Chang-An.,Zhao, Yong.,...&Chen, Ji-Jun.(2014).Synthesis, structure-activity relationships and biological evaluation of dehydroandrographolide and andrographolide derivatives as novel anti-hepatitis B virus agents.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,24(10),2353-2359. |
| MLA | Chen, Hao,et al."Synthesis, structure-activity relationships and biological evaluation of dehydroandrographolide and andrographolide derivatives as novel anti-hepatitis B virus agents".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 24.10(2014):2353-2359. |
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