吡喃半乳糖糖基化马蹄金素衍生物的合成及抗乙肝病毒活性研究
收稿日期: 2015-12-31
修回日期: 2016-03-10
网络出版日期: 2016-03-25
基金资助
国家自然科学基金（No.81360472）和西部之光人才（2014年）资助项目.
Synthesis and Anti-Hepatitis B Virus Activities of Galactopyranosyl Derivatives of Matijin-Su
Received date: 2015-12-31
Revised date: 2016-03-10
Online published: 2016-03-25
Supported by
Project supported by the National Natural Science Foundation of China (No. 81360472) and the Western Light Talent Culture Project (2014).
徐广灿 , 刘青川 , 袁洁 , 胡占兴 , 马芳芳 , 梁光义 , 徐必学 . 吡喃半乳糖糖基化马蹄金素衍生物的合成及抗乙肝病毒活性研究[J]. 有机化学, 2016 , 36(7) : 1617 -1625 . DOI: 10.6023/cjoc201512051
To improve the concentration in liver lesion tissue and increase the anti-hepatitis B virus (HBV) activities of Matijin-Su (MTS) derivatives, five hepatic targeting galactopyranosyl derivatives of MTS were synthesized by indirect connecting the liver targeting galactose ligands to MTS using ethanolamin as a linker and their structures were confirmed by 1H NMR, 13CNMR, 1H-1H COSY, HMQC and ESI-MS. The anti-HBV activities of those compounds were evaluated in HepG2 2.2.15 cells. The screening results showed that all target compounds had inhibitory effect on HBV DNA replication in HepG2 2.2.15 cells in a dose-response manner.
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