用于靶向递送至肿瘤的新型紫杉烷类化合物的合成及生物学评价
Synthesis and biological evaluation of novel taxoids designed for targeted delivery to tumors.
作者信息
Baloglu Erkan, Miller Michael L, Roller Elizabeth E, Cavanagh Emily E, Leece Barbara A, Goldmacher Victor S, Chari Ravi V J
机构信息
ImmunoGen, Inc., 128 Sidney Street, Cambridge, MA 02139, USA.
出版信息
Bioorg Med Chem Lett. 2004 Dec 6;14(23):5885-8. doi: 10.1016/j.bmcl.2004.09.025.
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.
使用药物-抗体偶联物提供了一种将抗癌药物特异性递送至癌细胞的方法。单独的单克隆抗体通常不具有高治疗效果，然而，它们能够选择性地靶向肿瘤标志物。我们已经制备出了细胞毒性比紫杉醇和多西他赛显著更高的紫杉烷类化合物。这些紫杉烷类化合物现在满足了在使用单克隆抗体的靶向递送方法中所需的高效能。本文报道了这些紫杉烷类化合物的合成及生物学评价。
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