Synthesis of a novel tri-antennary galactoside with high hepatocyte targeting

Synthesis of a novel tri-antennary galactoside with high hepatocyte targeting
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DOI:
10.1016/j.cclet.2007.03.018
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发表时间:
2007-05
影响因子:
9.1
通讯作者:
Lei Tang;Yong Wu;Jiao Lu;Zhirong Zhang;J. Yang;Li Hai
Lei Tang;Yong Wu;Jiao Lu;Zhirong Zhang;J. Yang;Li Hai
中科院分区:
化学1区
文献类型:
--
作者:
Lei Tang;Yong Wu;Jiao Lu;Zhirong Zhang;J. Yang;Li Hai

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以硫代半乳糖苷簇为靶向配体,合成了一种新型双功能化合物,用于肝细胞基因转染。四触角树状-OMs 45被用作三个半乳糖苷的附着的支架,而另一个甲磺酸酯末端通过聚(乙二醇)链与胆固醇连接。该设计为双功能化合物的合成提供了一个有效的途径。
A novel bifunctional compound carrying cluster thiogalactoside as the cell targeting ligands was synthesized for gene delivery to hepatocytes. Tetra-antennary dendr-OMs45 was used as a scaffold for the attachment of three galactosides, while the other mesylate end was linked with cholesterol through poly(ethylene glycol) chain. This design provided an effective entry for the synthesis of the bifunctional compound.