前药
阿霉素
细胞毒性
化学
羟甲基
水解
药理学
化疗
组合化学
生物化学
立体化学
医学
体外
内科学
作者
S. Desbene,Van Liew Hd,Serge Michel,Marion Koch,F. Tillequin,George A. Fournier,N Farjaudon,Claude Monneret
出处
期刊:PubMed
日期:1998-12-01
卷期号:13 (8): 955-68
被引量:2
摘要
The three new hydrophilic prodrugs 2, 3 and 4 have been prepared from methyl (4-hydroxymethyl-2-nitrophenyl 2,3,4-tri-O-acetyl-beta-D-glucopyranosid)uronate (5) and doxorubicin. Their low cytotoxicity, efficient release of doxorubicin after hydrolysis by beta-D-glucuronidase, and in the cases of 2 and 3 stability at pH 7.2 fulfil the preliminary requirement for their use in antibody-directed enzyme prodrug therapy or prodrug monotherapy.
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