Parallel Synthesis and Biological Evaluation of Destruxin E Analogs Modified with a Side Chain in the α-Hydroxycarboxylic Acid Moiety

Masahito Yoshida, Kenta Adachi, Hayato Murase, Hiroshi Nakagawa, Takayuki Doi

研究成果: Article査読

1 被引用数 (Scopus)

抄録

This study demonstrates the synthesis and biological evaluation of destruxin E analogs possessing various functional groups in the α-hydroxycarboxylic acid moiety. Parallel synthesis of eleven analogs was successfully achieved through solution-phase peptide synthesis and macrolactonization. Biological evaluation of the synthetic analogs using osteoclast-like multi nuclear cells (OCLs) revealed that the epoxide group in the side chain of α-hydroxycarboxylic acid and the orientation of the oxygen atom are essential factors in the desired potent activity that induces morphological changes in OCLs for the inhibition of bone-resorbing activity.

本文言語English
ページ(範囲)1669-1676
ページ数8
ジャーナルEuropean Journal of Organic Chemistry
2019
7
DOI
出版ステータスPublished - 2019 2 21

ASJC Scopus subject areas

  • 物理化学および理論化学
  • 有機化学

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