On the Total Synthesis and Preliminary Biological Evaluations of 15( R ) and 15( S ) Aza-dEpoB: A Mitsunobu Inversion at C15 in Pre-Epothilone Fragments
2000; American Chemical Society; Volume: 2; Issue: 11 Linguagem: Inglês
10.1021/ol005932m
ISSN1523-7060
AutoresShawn J. Stachel, Mark D. Chappell, Chul Bom Lee, Samuel J. Danishefsky, Ting‐Chao Chou, Lifeng He, Susan Band Horwitz,
Tópico(s)Synthetic Organic Chemistry Methods
ResumoThe syntheses of two epothilone analogues, 15(S)-aza-12,13-desoxyepothilone B and the epimeric 15(R)-aza-12,13-desoxyepothilone B, are described. A Mitsunobu inversion was utilized for elaboration of pre-epothilone fragments to the corresponding macrolactam. Tubulin binding and cytotoxicity profiles of these analogues are presented.
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