Design, Synthesis, and Biological Activity of Isosyringolin A

详细信息    查看全文

• 作者：Shun Kitahata ; Takuya Chiba ; Takashi Yoshida ; Masaki Ri ; Shinsuke Iida ; Akira Matsuda ; Satoshi Ichikawa
• 刊名：Organic Letters
• 出版年：2016
• 出版时间：May 6, 2016
• 年：2016
• 卷：18
• 期：9
• 页码：2312-2315
• 全文大小：282K
• 年卷期：0
• ISSN：1523-7052

文摘

Isosyringolin A, which is an isomer of the proteasome-inhibiting natural product syringolin A, was designed and synthesized to develop analogues that are step economical and synthetically accessible in a practical manner. It was revealed that isosyringolin A exhibited proteasome-inhibitory activity comparable to that of syringolin A and that its derivatization leads to great enhancement in its proteasome inhibitory activity as well as its cytotoxicity against human myeloma cells.