Synthesis of Doxorubicin Conjugates Through 14-Hydroxy Group to Melanotransferrin P97

Abstract

Using Fmoc to protect the amino group, Fmoc-doxorubicin is conjugated through the 14-hydroxy group to the amino group of melanotransferrin p97 by spacer arms such as succinate and glutarate. The Fmoc group is then removed under basic conditions, which affords doxorubicin-p97 conjugates. The resulting bioconjugates are potential agents for treating brain tumors.

Keywords:

• Doxorubicin
• Bioconjugate
• Protein carrier
• Cross-linking
• Blood-brain barrier
• Drug delivery
• Anticancer drug
• Brain tumor
• Ester bond linkage

Acknowledgments

We are grateful to Dr. Pascale Tiger, Dr. Malcolm Kennard, and Dr. Gavin Arthur for their helpful discussions.