|
|||||
|
|
Synthesis and biological activity of [Tic] didemnin B |
|
| Authors: | Amy J. Pfizenmayer,Matthew D. Vera,Xiaobin Ding,Dong Xiao,Wei-Chuan Chen,Madeleine M. Joullié ,Deepika Tandon,Peter L. Toogood |
| Affiliation: | a Department of Chemistry, University of Pennsylvania, 231 S. 34th St., Philadelphia, PA 19104-6323, U.S.A. b Department of Chemistry, University of Michigan, Ann Arbor, MI 48109-1055, U.S.A. |
| Abstract: | A didemnin B analog containing a Tic (1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid) as a conformationally restrained replacement for tyrosine has been synthesized and shown to have comparable potency as a protein biosynthesis inhibitor. Synthetic highlights include an oxidation of an alcohol to an acid in the presence of the sensitive Tic heterocycle and a modified Schmidt-type one-pot macrocyclization. |
| Keywords: | |
| 本文献已被 ScienceDirect 等数据库收录！ | |