Synthesis of potent taxoids for tumor-specific delivery using monoclonal antibodies

被引:14
作者
Miller, ML
Roller, EE
Wu, XY
Leece, BA
Goldmacher, VS
Chari, RVJ
Ojima, I
机构
[1] ImmunoGen Inc, Cambridge, MA 02139 USA
[2] SUNY Stony Brook, Dept Chem, Stony Brook, NY 11794 USA
关键词
taxoid; antibody conjugate; tumor specific; targeted delivery;
D O I
10.1016/j.bmcl.2004.05.027
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The targeted delivery of taxoids, in the form of taxane-antibody immunoconjugates, requires the preparation of taxoids containing moieties suitable for their conjugation to monoclonal antibodies. A series of taxoids incorporating a disulfide-containing linker at various positions of the taxoid framework have been prepared to investigate the most suitable position for conjugation. A second series of taxoids modified at the C-2 position aimed at increasing the potency of these taxanes has also been prepared. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:4079 / 4082
页数:4
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