Synthesis of doxorubicin conjugates through 14-hydroxy group to melanotransferrin p97

被引：9

作者：

Chen, QQ ^{[1
]}

Sowa, DA ^{[1
]}

Gabathuler, R ^{[1
]}

机构：

[1] Biomarin Pharmaceut Inc, Novato, CA 94949 USA

来源：

SYNTHETIC COMMUNICATIONS | 2003年 / 33卷 / 14期

关键词：

doxorubicin; bioconjugate; protein carrier; crosslinking; blood-brain barrier; drug delivery; anticancer drug; brain tumor; ester bond linkage;

D O I：

10.1081/SCC-120021828

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

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.

引用

页码：2391 / 2400

页数：10

共 28 条

[1]

ARCAMONE F, 1981, DOXORUBICIN ANTICANC, pCH2

[2]

Begley DJ, 2000, BLOOD-BRAIN BARRIER AND DRUG DELIVERY TO THE CNS, P93

[3] Synthesis of doxorubicin conjugates through hydrazone bonds to melanotransferrin p97 [J].