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Synthesis and in vitro anti-hepatitis B virus activity of six-membered azanucleoside analogues
Wang, Dan1; Li, Yu-Huan2,3; Wang, Yu-Ping2,3; Gao, Rong-Mei2,3; Zhang, Li-He1; Ye, Xin-Shan1
关键词Azanucleoside Azasugar Hepatitis b Virus Anti-viral Agent Synthesis
刊名BIOORGANIC & MEDICINAL CHEMISTRY
2011
DOI10.1016/j.bmc.2010.11.063
19期:1页:41-51
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Biochemistry & Molecular Biology ; Chemistry, Medicinal ; Chemistry, Organic
研究领域[WOS]Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
关键词[WOS]CARBOCYCLIC NUCLEOSIDES ; BIOLOGICAL-ACTIVITY ; DERIVATIVES ; REPLICATION
英文摘要

Fifteen novel six-membered azanucleoside derivatives were prepared and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in human hepatoblastoma-derived liver Hep-G2 cells. The most potent compound 16b with an IC50 value of 2.74 mu g/mL (lower than 3TC) and a SI value of 13.5 was disclosed. The key synthetic steps involved the rearrangement of lactones (which were readily obtained from monosaccharides) and the Lewis acid-catalyzed condensation of nucleobases with azasugar donors. Using the versatile acetylated azasugar donors, azanucleosides covering three types of azasugars and four types of natural nucleobases were successfully obtained. The experimental results showed that some six-membered azanucleosides may find applications in the discovery of new anti-viral agents. (C) 2010 Elsevier Ltd. All rights reserved.

语种英语
WOS记录号WOS:000285724800004
项目编号90713010 ; 2009ZX09501-011
资助机构National Natural Science Foundation of China ; Ministry of Science and Technology of China
引用统计
被引频次:6[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/400002259/56776
专题北京大学药学院
北京大学药学院_药物化学系
作者单位1.Peking Univ, State Key Lab Nat & Biomimet Drugs, Sch Pharmaceut Sci, Beijing 100191, Peoples R China
2.Chinese Acad Med Sci, Inst Med Biotechnol, Beijing 100050, Peoples R China
3.Peking Union Med Coll, Beijing 100050, Peoples R China
推荐引用方式
GB/T 7714
Wang, Dan,Li, Yu-Huan,Wang, Yu-Ping,et al. Synthesis and in vitro anti-hepatitis B virus activity of six-membered azanucleoside analogues[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2011,19(1):41-51.
APA Wang, Dan,Li, Yu-Huan,Wang, Yu-Ping,Gao, Rong-Mei,Zhang, Li-He,&Ye, Xin-Shan.(2011).Synthesis and in vitro anti-hepatitis B virus activity of six-membered azanucleoside analogues.BIOORGANIC & MEDICINAL CHEMISTRY,19(1),41-51.
MLA Wang, Dan,et al."Synthesis and in vitro anti-hepatitis B virus activity of six-membered azanucleoside analogues".BIOORGANIC & MEDICINAL CHEMISTRY 19.1(2011):41-51.
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