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

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 resultin...

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Published in:Synthetic communications 2003-01, Vol.33 (14), p.2391-2400
Main Authors: Chen, Qingqi, Sowa, Damian A., Gabathuler, Reinhard
Format: Article
Language:English
Subjects:
Anticancer drug
Bioconjugate
Blood-brain barrier
Brain tumor
Cross-linking
Doxorubicin
Drug delivery
Ester bond linkage
Protein carrier
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cited_by cdi_FETCH-LOGICAL-c284t-491174dd53d6f7196bf7cb41663c104c1068ec6374de05f4d866a447a3f1e0723
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description 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.
doi_str_mv 10.1081/SCC-120021828
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subjects Anticancer drug
Bioconjugate
Blood-brain barrier
Brain tumor
Cross-linking
Doxorubicin
Drug delivery
Ester bond linkage
Protein carrier
title Synthesis of Doxorubicin Conjugates Through 14-Hydroxy Group to Melanotransferrin P97
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