Novel Notch-sparing γ-secretase inhibitors derived from a peroxisome proliferator-activated receptor agonist library

Motonori Kurosumi, Yoshino Nishio, Satoko Osawa, Hisayoshi Kobayashi, Takeshi Iwatsubo, Taisuke Tomita, Hiroyuki Miyachi

Research output: Contribution to journalArticlepeer-review

6 Citations (Scopus)

Abstract

Screening of our library of peroxisome proliferator-activated receptor (PPAR) agonists yielded several phenylpropanoic acid-derived γ-secretase inhibitors (GSIs). Structure-activity relationship studies indicated that (R)-configuration of α-substituted phenylpropanoic acid structure and cinnamic acid structure is favorable to prepare Notch-sparing GSIs.

Original languageEnglish
Pages (from-to)5282-5285
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number17
DOIs
Publication statusPublished - Sep 1 2010

Keywords

  • Notch-sparing γ-secretase inhibitor
  • PPAR
  • γ-Secretase
  • γ-Secretase inhibitor

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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