A daunorubicin β-galactoside prodrug for use in conjunction with gene-directed enzyme prodrug therapy

被引：30

作者：

Ghosh, AK ^{[1
]}

Khan, S ^{[1
]}

Marini, F ^{[1
]}

Nelson, JA ^{[1
]}

Farquhar, D ^{[1
]}

机构：

[1] Univ Texas, MD Anderson Canc Ctr, Dept Expt Therapeut, Houston, TX 77030 USA

来源：

TETRAHEDRON LETTERS | 2000年 / 41卷 / 25期

基金：

美国国家卫生研究院;

关键词：

anthracycline; daunomycin; prodrug; beta-galactosidase; gene therapy;

D O I：

10.1016/S0040-4039(00)00742-5

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

N-[4-(beta-D-Galactopyranosyl)-3-nitrobenzyloxycarbonyl]daunomycin was synthesized as a neutral prodrug of daunomycin. Although stable in 0.05 M phosphate buffer, pH 7.4 at 37 degrees C, it was rapidly converted to daunomycin and 3-nitro-4-hydroxybenzyl alcohol under the same conditions in the presence of E. coli beta-galactosidase. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：4871 / 4874

页数：4

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