Design, total synthesis, and evaluation of novel open-chain epothilone analogues
Design, total synthesis, and evaluation of novel open-chain epothilone analogues
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DOI：
10.1021/ol0528787
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发表时间：
2006-02-16
期刊：
影响因子：
5.2
通讯作者：
Tillekeratne, LMV
中科院分区：
文献类型：
--
作者：
Alhamadsheh, MM;Hudson, RA;Tillekeratne, LMV
设计、全合成并评价了两个含C1-C8关键片段和芳香侧链的埃博霉素类似物。生物学评价显示，柔性C1-C8区域和分子支架之间的进一步限制对于有效抑制细胞增殖可能是必要的。
The design, total synthesis, and biological evaluation of two open-chain analogues of epothilone incorporating the critical C1-C8 fragment and the aromatic side chain held together by a small molecular scaffold have been achieved. Biological evaluation revealed that further restraint between the flexible C1-C8 region and the molecular scaffold may be necessary for potent inhibition of cell proliferation.