Synthesis and antitumor activity of novel C-7 paclitaxel ethers: Discovery of BMS-184476
Synthesis and antitumor activity of novel C-7 paclitaxel ethers: Discovery of BMS-184476
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DOI：
10.1021/jm0102607
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发表时间：
2001-12-20
影响因子：
7.3
通讯作者：
Wittman, MD
中科院分区：
文献类型：
--
作者：
Altstadt, TJ;Fairchild, CR;Wittman, MD
介绍了C-7紫杉醇醚的制备方法。通过活化相应的甲硫基甲基醚，然后加入醇，制备各种取代的醚。C-7醚基以及3'侧链位置的变化导致发现了一种新型紫杉烷BMS-184476（4），其临床前抗肿瘤活性上级于紫杉醇。
The preparation of C-7 paclitaxel ethers is described. Various substituted ethers were prepared via activation of the corresponding methylthiomethyl ether followed by alcohol addition. Variation of the C-7 ether group as well the 3' side chain position led to the discovery of a novel taxane, BMS-184476 (4), with preclinical antitumor activity superior to paclitaxel.