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
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.
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页码:3347 / 3352
页数:6
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