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First enzymatically activated Taxotere prodrugs designed for ADEPT and PMT.

Abstract：

:Described here are the syntheses and preliminary biological evaluations of the first two enzymatically activated prodrugs of docetaxel (Taxotere) 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.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Bouvier E,Thirot S,Schmidt F,Monneret C

doi

10.1016/j.bmc.2003.12.013

subject

Has Abstract

pub_date

2004-03-01 00:00:00

pages

969-77

issue

5

eissn

0968-0896

issn

1464-3391

pii

S0968089603008745

journal_volume

12

pub_type

杂志文章

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