|
|||||
|
|
A solid-phase total synthesis of the cyclic depsipeptide HDAC inhibitor spiruchostatin A |
|
| Authors: | Yusuke Iijima Kazuo Shin-ya Takayuki Doi Takashi Takahashi |
| Institution: | a Department of Applied Chemistry, Tokyo Institute of Technology, 2-12-1, Ookayama, Meguro, Tokyo 152-8552, Japan b Japan Biological Informatics Consortium (JBIC), 2-45 Aomi, Koto-ku, Tokyo 135-8073, Japan c National Institute of Advanced Industrial Science and Technology, 2-42, Aomi, Koto-ku, Tokyo 135-0064, Japan d School of Chemistry, University of Southampton, Southampton SO17 1BJ, United Kingdom e Graduate School of Pharmaceutical Sciences, Tohoku University, Aza-Aoba, Aramaki, Aoba, Sendai 980-8578, Japan |
| Abstract: | Spiruchostatin A, a potent histone deacetylase inhibitor, was efficiently synthesized from (3S,4R)-4-amino-3-hydroxy-5-methylhexanoic acid utilizing solid-phase peptide elongation with d-cysteine, d-alanine, and (E)-3-hydroxy-7-thio-4-heptenoic acid and solution-phase macrolactonization, followed by intramolecular disulfide formation. |
| Keywords: | Cyclic depsipeptide Histone deacetylase Natural product synthesis Solid-phase synthesis |
| 本文献已被 ScienceDirect 等数据库收录！ | |