Novel C2–C3′ N-peptide linked macrocyclic taxoids. Part 1: Synthesis and biological activities of docetaxel analogues with a peptide side chain at C3′
- 作者：Anne-Laure Larroque ; Joë ; lle Dubois ; Sylviane Thoret ; Geneviè ; ve Aubert ; Daniel Gué ; nard and Franç ; oise Gué ; ritte
- 关键词：Microtubules ; Docetaxel ; Paclitaxel ; Taxoids
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2005
- 期刊代码：10_0960894x
- 类别：ch
- 出版时间：2005
- 卷：15
- 期：21
- 页码：4722-4726
- 文件大小：298 K
摘要
A series of novel docetaxel analogues possessing a peptide side chain at the C3′-N position was synthesized. These compounds were designed to mimic a region of the α-tubulin loop that is equivalent to the paclitaxel binding pocket in β-tubulin. Eight new peptidic taxoids were obtained and evaluated as inhibitors of microtubule disassembly, as well as for their cytotoxicity.