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Synthetic Communications
An International Journal for Rapid Communication of Synthetic Organic Chemistry
Volume 36, 2006 - Issue 18
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Original Articles

Synthesis of Cholesterylated Thiogalactosides for Gene Delivery

Li Hai Key Laboratory of Drug Target, West China School of Pharmacy, Sichuan University, Chengdu, Sichuan, China
,
Jiang Fan Key Laboratory of Drug Target, West China School of Pharmacy, Sichuan University, Chengdu, Sichuan, China
,
Zhirong Zhang Key Laboratory of Drug Target, West China School of Pharmacy, Sichuan University, Chengdu, Sichuan, China
,
Guoyao Zhang Key Laboratory of Drug Target, West China School of Pharmacy, Sichuan University, Chengdu, Sichuan, China
&
Yong Wu Key Laboratory of Drug Target, West China School of Pharmacy, Sichuan University, Chengdu, Sichuan, China
Pages 2633-2648 | Received 07 Jan 2006, Published online: 16 Feb 2007
 
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Abstract

A series of cholesterylated thiogalactosides L1 –L6 the cell targeting ligands for gene delivery to hepatocytes, was synthesized. Related poly(ethylene glycol) chain was used as a bridge for the attachment of galactoside on one hydroxyl end, while the other hydroxyl end was linked with cholesterol. This design provided an effective entry for the synthesis of a poly(ethylene glycol) compound with the hepatocyte targeting.

Acknowledgment

This work was funded by the National High Technology Research and Development Program of China (863 program, No. 2001AA218021) and Ministry of Education of China (No. 20050610085).

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