Synthesis and biological activity of novel epothilone aziridines.
Synthesis and biological activity of novel epothilone aziridines.
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DOI：
10.1021/ol016273w
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发表时间：
2001-07
期刊：
影响因子：
5.2
通讯作者：
Alicia Regueiro-Ren;R. Borzilleri;Xiaoping Zheng;Soong-Hoon Kim;James A. Johnson;Craig R. Fairchild;Francis Y. F. Lee;Byron H. Long;G. Vite
中科院分区：
文献类型：
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作者：
Alicia Regueiro-Ren;R. Borzilleri;Xiaoping Zheng;Soong-Hoon Kim;James A. Johnson;Craig R. Fairchild;Francis Y. F. Lee;Byron H. Long;G. Vite
[reaction: see text]. A series of 12alpha,13alpha-aziridinyl epothilone derivatives were synthesized in an efficient manner from epothilone A. The final semisynthetic route involves a formal double-inversion of stereochemistry at both the C12 and C13 positions. All aziridine analogues were tested for effects on tubulin binding polymerization and cytotoxicity. The results indicate that the aziridine moiety is a viable isosteric replacement for the epoxide in the case of epothilones.
