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
资助信息West Light Foundation of the Chinese Academy of Sciences; National Science Foundation of China [81025023]; International Foundation for Science in Sweden [F/5202-1]; National Natural Science Foundation of China [81202436]; Youth Innovation Promotion Association, CAS
收录类别SCI
语种英语
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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
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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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