First enzymatically activated Taxotere prodrugs designed for ADEPT and PMT

被引：26

作者：

Bouvier, E ^{[1
]}

Thirot, S ^{[1
]}

Schmidt, F ^{[1
]}

Monneret, C ^{[1
]}

机构：

[1] Inst Curie, UMR176 CNRS, Sect Rech, Paris 05, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2004年 / 12卷 / 05期

基金：

澳大利亚研究理事会;

关键词：

Taxotere; docetaxel; prodrug; ADEPT;

D O I：

10.1016/j.bmc.2003.12.013

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Described here are the syntheses and preliminary biological evaluations of the first two enzymatically activated prodrugs of docetaxel (Taxotere(R)) reported to date. These prodrugs were designed as potential candidates for selective chemotherapy in ADEPT or PMT. They are constituted of a glucuronic acid moiety, a double spacer and the cytotoxic drug, differing only by the spacer substitution. The prodrugs were stable in a buffer, and the in vitro studies showed good detoxification and hydrolysis kinetics. As docetaxel was efficiently released in both cases, these compounds are very valuable candidates for further biological evaluations. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：969 / 977

页数：9

共 18 条

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