Synthesis of hemslecin A derivatives: A new class of hepatitis B virus inhibitors
Guo, Rui-Hua1; Geng, Chang-An1; Huang, Xiao-Yan1; Ma, Yun-Bao1; Zhang, Quan1; Wang, Li-Jun1; Zhang, Xue-Mei1; Zhang, Rong-Ping2; Chen, Ji-Jun1
通讯作者Zhang, RP (reprint author), Kunming Med Univ, Kunming 650500, Yunnan, Peoples R China.,zhrpkm@163.com ; chenjj@mail.kib.ac.cn
2013-03-01
发表期刊BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN0960-894X
卷号23期号:5页码:1201-1205
摘要A series of hemslecin A derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activities, namely, inhibiting the secretion of hepatitis B surface antigen (HBsAg), hepatitis B e antigen (HBeAg), and HBV DNA replication on HepG 2.2.15 cells. Most of the derivatives showed enhanced anti-HBV activities, of which compounds A1-A7, B5, C and E exhibited significant activities inhibiting HBV DNA replication with IC50 values of 2.8-11.6 mu M, comparable to that of the positive control, tenofovir. Compounds A1-A3, A5, B5, and C displayed low cytotoxicities, which resulted in high SI values of 89.7, 55.6, 77.8, >83.4, >55.8, and >150.5, respectively. Crown Copyright (C) 2013 Published by Elsevier Ltd. All rights reserved.
关键词Hemslecin a Derivatives Hepatitis b Virus
学科领域Pharmacology & Pharmacy ; Chemistry
DOI10.1016/j.bmcl.2013.01.024
收录类别SCI ; IC
语种英语
WOS记录号WOS:000314693400008
引用统计
文献类型期刊论文
条目标识符http://ir.kib.ac.cn/handle/151853/16222
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, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources W China, Kunming 650204, Peoples R China
2.Kunming Med Univ, Kunming 650500, Yunnan, Peoples R China
推荐引用方式
GB/T 7714
Guo, Rui-Hua,Geng, Chang-An,Huang, Xiao-Yan,et al. Synthesis of hemslecin A derivatives: A new class of hepatitis B virus inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2013,23(5):1201-1205.
APA Guo, Rui-Hua.,Geng, Chang-An.,Huang, Xiao-Yan.,Ma, Yun-Bao.,Zhang, Quan.,...&Chen, Ji-Jun.(2013).Synthesis of hemslecin A derivatives: A new class of hepatitis B virus inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,23(5),1201-1205.
MLA Guo, Rui-Hua,et al."Synthesis of hemslecin A derivatives: A new class of hepatitis B virus inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 23.5(2013):1201-1205.
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