A new spacer group derived from arylmalonaldehydes for glucuronylated prodrugs

被引：16
作者：
Papot, S
Combaud, D
Gesson, JP
机构：
[1] Univ Poitiers, Lab Chim 12, F-86022 Poitiers, France
[2] CNRS, F-86022 Poitiers, France
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 18期
关键词：
D O I：
10.1016/S0960-894X(98)00454-5
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A new glucuronylated prodrug of doxorubicin, potentially useful for ADEPT or PMT cancer chemotherapy, has been prepared from 4-methyl phenyl malonaldehyde. The enol ether spacer, linked via a carbamate to the 3'-amino group of doxorubicin is rapidly cleaved after beta-glucuronidase (E coli) catalyzed hydrolysis at pH 7.2 and 37 degrees C. (C) 1998 Elsevier Science Ltd. All rights reserved.
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页码：2545 / 2548
页数：4
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