Synthesis and Anti-HBV Evaluation of 5-Halogenated 2'-Deoxy-2'-β-fluoro-4'-azido Pyrimidine Nucleosides

被引：3
|
作者：
Guo, Meichao [1 ]
Kang, Jinfeng [1 ]
Hou, Jiao [1 ]
Zhang, Qianqian [1 ]
Yu, Wenquan [1 ]
Chang, Junbiao [1 ,2 ]
机构：
[1] Zhengzhou Univ, Coll Chem, Zhengzhou 450001, Peoples R China
[2] Henan Normal Univ, Sch Chem & Chem Engn, Henan Key Lab Organ Funct Mol & Drug Innovat, Xinxiang 453007, Henan, Peoples R China
来源：
CHINESE JOURNAL OF ORGANIC CHEMISTRY | 2020年 / 40卷 / 01期
基金：
中国国家自然科学基金;
关键词：
5-halogenated; pyrimidine nucleoside; synthesis; anti-HBV activity; BIOLOGICAL EVALUATION; ANALOGS; FNC;
D O I：
10.6023/cjoc201907054
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
A series of 5-halogenated 2'-deoxy-2'-beta-fluoro-4'-azido pyrimidine nucleosides were synthesized from m-chlorobenzoyl protected 2'-deoxy-2'-beta-fluoro-4'-azido uridine via ammonium cerium nitrate (CAN)-mediated halogenation, activation by triazole, amination, and deprotection. In vitro biological evaluation demonstrated that 5-chloro (6a) and 5-iodo (6c) nucleoside derivatives possess potent anti-HBV (hepatitis B virus) activity with low cytotoxicity.
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收藏
页码：221 / 225
页数：5
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