Synthesis of erythrocentaurin derivatives as a new class of hepatitis B virus inhibitors | |
Geng, Chang-An; Huang, Xiao-Yan; Ma, Yun-Bao; Zhang, Xue-Mei; Chen, Ji-Jun; Chen,JJ (reprint author),Chinese Acad Sci,Kunming Inst Bot,State Key Lab Phytochem & Plant Resources West Ch,Kunming 650201,Peoples R China.; chenjj@mail.kib.ac.cn | |
2015-04-01 | |
发表期刊 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS |
卷号 | 25期号:7页码:1568-1571 |
摘要 | Twenty-four derivatives of erythrocentaurin (ET) were synthesized and evaluated for their anti-HBV activities on HepG 2.2.15 cell line in vitro. Eight compounds 1, 2, 5, 8, 9, 1e, 1k, and 1m increased activity against HBV DNA replication with the SI values higher than 11. In particular, derivatives 1e and 1k exhibited the most potent inhibition on HBV DNA replication with the IC50 values of 0.026 mM (SI > 70.8) and 0.045 mM (SI > 36.0), respectively. The primary structure-activity relationships (SARs) of ET derivatives were summarized for exploring potent anti-HBV agents. (C) 2015 Elsevier Ltd. All rights reserved. |
关键词 | Erythrocentaurin Anti-hbv Activity Structure-activity Relationships |
学科领域 | Chemistry, Medicinal ; Chemistry, Organic |
DOI | 10.1016/j.bmcl.2015.02.009 |
收录类别 | SCI |
语种 | 英语 |
WOS记录号 | WOS:000351688700040 |
引用统计 | |
文献类型 | 期刊论文 |
条目标识符 | http://ir.kib.ac.cn/handle/151853/20583 |
专题 | 植物化学与西部植物资源持续利用国家重点实验室 |
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.; chenjj@mail.kib.ac.cn |
作者单位 | Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Peoples R China |
推荐引用方式 GB/T 7714 | Geng, Chang-An,Huang, Xiao-Yan,Ma, Yun-Bao,et al. Synthesis of erythrocentaurin derivatives as a new class of hepatitis B virus inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2015,25(7):1568-1571. |
APA | Geng, Chang-An.,Huang, Xiao-Yan.,Ma, Yun-Bao.,Zhang, Xue-Mei.,Chen, Ji-Jun.,...&chenjj@mail.kib.ac.cn.(2015).Synthesis of erythrocentaurin derivatives as a new class of hepatitis B virus inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,25(7),1568-1571. |
MLA | Geng, Chang-An,et al."Synthesis of erythrocentaurin derivatives as a new class of hepatitis B virus inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 25.7(2015):1568-1571. |
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