Cathepsin B-sensitive dipeptide prodrugs.: 2.: Models of anticancer drugs paclitaxel (Ttaxol®), mitomycin C and doxorubicin

被引：96

作者：

Dubowchik, GM ^{[1
]}

Mosure, K ^{[1
]}

Knipe, JO ^{[1
]}

Firestone, RA ^{[1
]}

机构：

[1] Bristol Myers Squibb Co, Pharmaceut Res Inst, Wallingford, CT 06492 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 23期

关键词：

D O I：

10.1016/S0960-894X(98)00610-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Substrates containing doxorubicin (DOX), paclitaxel (taxol(R)), and mitomycin C (MMC) attached to the cathepsin B-sensitive dipeptide Phe-Lys via a self-immolative spacer were prepared as model compounds for internalizing anticancer immunoconjugates. Cathepsin B-mediated release rates of free drug, rat liver lysosomal susceptibility and human plasma stability were measured for each. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：3347 / 3352

页数：6

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