Synthesis and biological evaluation of novel taxoids designed for targeted delivery to tumors

被引：16

作者：

Baloglu, E ^{[1
]}

Miller, ML ^{[1
]}

Roller, EE ^{[1
]}

Cavanagh, EE ^{[1
]}

Leece, BA ^{[1
]}

Goldmacher, VS ^{[1
]}

Chari, RVJ ^{[1
]}

机构：

[1] ImmunoGen Inc, Cambridge, MA 02139 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 23期

关键词：

taxol; taxotere; paclitaxel; docetaxel; taxane; cancer; monoclonal antibody;

D O I：

10.1016/j.bmcl.2004.09.025

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The use of drug-antibody conjugates affords a method for the targeted delivery of anticancer drugs specifically to cancer cells. Monoclonal antibodies alone usually do not possess high therapeutic efficacy, however, they are capable of targeting tumor markers selectively. We have prepared taxoids with significantly higher cytotoxicity than paclitaxel and docetaxel. These taxoids now meet the high potency required for use in a targeted-delivery approach using monoclonal antibodies. The synthesis and biological evaluation of these taxoids are reported. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：5885 / 5888

页数：4

共 28 条

[1]

[Anonymous], 1995, Taxol: Sci. Appl

[2] Synthesis and biological evaluation of C-3′NH/C-10 and C-2/C-10 modified paclitaxel analogues [J].