Synthesis of Cholesterylated Thiogalactosides for Gene Delivery

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.

Keywords:

• Cholesterylated thiogalactoside
• gene delivery
• poly(ethylene glycols) (PEG)
• targeting ligand

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).