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学科主题: 药学
题名:
Synthesis and biological evaluation of ring A and/or C expansion and opening echinocystic acid derivatives for anti-HCV entry inhibitors
作者: 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
发表日期: 2015-09-18
DOI: 10.1016/j.ejmech.2015.08.034
卷: 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
所属项目编号: 2010CB912300 ; 81361168002 ; 81373271 ; 81101239 ; 81202975
项目资助者: National Basic Research Program of China (973 Program) ; National Natural Science Foundation of China
WOS记录号: WOS:000361922600049
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/57111
Appears in Collections:北京大学药学院_期刊论文

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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

Recommended Citation:
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.
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