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 |
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| Authors: | Stachel S J Chappell M D Lee C B Danishefsky S J Chou T C He L Horwitz S B |
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| Affiliation: | Laboratories for Bioorganic Chemistryand Biochemical Pharmacology, Sloan-Kettering Institute for Cancer Research, New York, NY 10021, USA. |
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| Abstract: | [reaction-see text] The 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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