Solid-phase total synthesis of biologically active cyclodepsipeptide spiruchostatin A

Masahito Yoshida

Research output: Contribution to journalArticlepeer-review

Abstract

Cyclic peptides have been emerged as novel candidates for recent drug discovery, because cyclization or introduction of unnatural amino acid residues significantly improve physicochemical properties such as metabolic stability and cell permeability. Toward elucidation of the mode of action of cyclic peptides, we intensely investigated the structure-activity relationships study based on the total synthesis of naturally occurring cyclic peptides and its analogues utilizing solid-phase. Herein, we describe the details of total synthesis of spiruchostatin A, a potent histone deacetylase inhibitor, using a macrolactonization on the silyl-linked polymer-support.

Original languageEnglish
Pages (from-to)522-525
Number of pages4
JournalYuki Gosei Kagaku Kyokaishi/Journal of Synthetic Organic Chemistry
Volume76
Issue number5
DOIs
Publication statusPublished - 2018 Jan 1

Keywords

  • Cyclic peptide
  • Natural product
  • Solid-phase synthesis
  • Total synthesis

ASJC Scopus subject areas

  • Organic Chemistry

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