IR@PKUHSC  > 北京大学药学院  > 药学院
学科主题药学
Synthesis and biological evaluation of ring A and/or C expansion and opening echinocystic acid derivatives for anti-HCV entry inhibitors
Wang, Han1; Yu, Fei1,2; Peng, Yiyun1; Wang, Qi1; Han, Xu1; Xu, Renyang1; Zhou, Xiaoshu1; Wan, Chuanxing1,4; Fan, Zibo1; Jiao, Pingxuan1; Zhang, Yongmin3; Zhang, Lihe1; Zhou, Demin1; Xiao, Sulong1
关键词Echinocystic Acid Ring Expansion Ring Opening Hcv Entry Inhibitor
刊名EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
2015-09-18
DOI10.1016/j.ejmech.2015.08.034
102页:594-599
收录类别SCI ; IC
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Medicinal
研究领域[WOS]Pharmacology & Pharmacy
关键词[WOS]OLEANANE-TYPE TRITERPENES ; HEPATITIS-C ; OLEANOLIC ACID ; VIRUS-INFECTION ; DRUG DISCOVERY ; MORONIC ACID ; URSOLIC ACID ; STEM BARK ; SOFOSBUVIR ; FUTURE
英文摘要

Echinocystic acid (EA), a naturally occurring oleanane-type triterpene isolated from Dipsacus asperoides, was found to have anti-HCV entry activity in our previous study. Expansion of triterpene structural diversity, including the ring A and/or C expansion and opening, was performed. To elucidate the pharmacophore of EA, seven lactones (8, 16, 17, 24, 26, 35 and 41), three 3,28-dioic acids (9, 36 and 42) and two pentols (10 and 27) were synthesized. The anti-HCV entry activities of those derivatives, along with their parental compound EA and analogs alpha,beta-unsaturated ketone (18), were evaluated. All the products showed no improvement but detrimental effect on potency of EA. The results demonstrated that ring A and C of EA are highly conserved, indicating the steric effects of the rigid skeleton have a profound effect on the potency. (C) 2015 Elsevier Masson SAS. All rights reserved.

语种英语
WOS记录号WOS:000361922600049
项目编号2010CB912300 ; 81361168002 ; 81373271 ; 81101239 ; 81202975
资助机构National Basic Research Program of China (973 Program) ; National Natural Science Foundation of China
引用统计
被引频次:9[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/57111
专题北京大学药学院_药学院
北京大学药学院
北京大学药学院_药物化学系
作者单位1.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
2.Kunming Univ Sci & Technol, Fac Med, Kunming 650500, Peoples R China
3.Univ Paris 06, CNRS, UMR 8232, Inst Parisien Chim Mol, F-75005 Paris, France
4.Tarim Univ, Key Lab Protect & Utilizat Biol Resources Tarim B, Xinjiang Prod & Construct Grp, Alar 843300, Peoples R China
推荐引用方式
GB/T 7714
Wang, Han,Yu, Fei,Peng, Yiyun,et al. Synthesis and biological evaluation of ring A and/or C expansion and opening echinocystic acid derivatives for anti-HCV entry inhibitors[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2015,102:594-599.
APA Wang, Han.,Yu, Fei.,Peng, Yiyun.,Wang, Qi.,Han, Xu.,...&Xiao, Sulong.(2015).Synthesis and biological evaluation of ring A and/or C expansion and opening echinocystic acid derivatives for anti-HCV entry inhibitors.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,102,594-599.
MLA Wang, Han,et al."Synthesis and biological evaluation of ring A and/or C expansion and opening echinocystic acid derivatives for anti-HCV entry inhibitors".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 102(2015):594-599.
条目包含的文件
条目无相关文件。
个性服务
推荐该条目
保存到收藏夹
查看访问统计
导出为Endnote文件
谷歌学术
谷歌学术中相似的文章
[Wang, Han]的文章
[Yu, Fei]的文章
[Peng, Yiyun]的文章
百度学术
百度学术中相似的文章
[Wang, Han]的文章
[Yu, Fei]的文章
[Peng, Yiyun]的文章
必应学术
必应学术中相似的文章
[Wang, Han]的文章
[Yu, Fei]的文章
[Peng, Yiyun]的文章
相关权益政策
暂无数据
收藏/分享
所有评论 (0)
暂无评论
 

除非特别说明,本系统中所有内容都受版权保护,并保留所有权利。