SYNTHESIS OF MACROMOLECULAR MITOMYCIN-C DERIVATIVES

被引：23

作者：

DEMARRE, A ^{[1
]}

SOYEZ, H ^{[1
]}

SCHACHT, E ^{[1
]}

机构：

[1] STATE UNIV GHENT,DEPT ORGAN CHEM,BIOMAT RES GRP,B-9000 GHENT,BELGIUM

来源：

JOURNAL OF CONTROLLED RELEASE | 1994年 / 32卷 / 02期

关键词：

SYNTHESIS; MITOMYCIN C; PRODRUG;

D O I：

10.1016/0168-3659(94)90051-5

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A series of polymeric prodrugs of Mitomycin C (MMC) were prepared by coupling the drug via a tri- or tetrapeptide spacer onto poly-[N-5-(2-hydroxyethyl)-L-glutamine] (PHEG). In the first step MMC was linked to the peptide spacer. For preparing the oligopeptide-MMC derivatives N-Fmoc protected oligopeptide was activated as the pentafluorophenyl ester. After coupling with MMC the N-protective group can be removed under mild conditions. The spacer-MMC derivatives were finally coupled to 4-nitrophenyl chloroformate activated PHEG.

引用

页码：129 / 137

页数：9

共 38 条

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