Novel γ-secretase inhibitors discovered by library screening of in-house synthetic natural product intermediates

Yasuko Takahashi, Haruhiko Fuwa, Akane Kaneko, Makoto Sasaki, Satoshi Yokoshima, Hifumi Koizumi, Tohru Takebe, Toshiyuki Kan, Takeshi Iwatsubo, Taisuke Tomita, Hideaki Natsugari, Tohru Fukuyama

Research output: Contribution to journalArticle

22 Citations (Scopus)

Abstract

Screening of our in-house compound library comprised of intermediates of natural product synthesis projects resulted in discovering two novel γ-secretase inhibitors, which coincidently had similar moieties, that is, cyclohexenone and two aryl groups arranged on the core six-membered ring. Structure-activity relationship studies of these compounds were also developed.

Original languageEnglish
Pages (from-to)3813-3816
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number14
DOIs
Publication statusPublished - 2006 Jul 15

Keywords

  • Cyclohexenone
  • Inhibitor
  • Structure-activity relationships
  • γ-Secretase

ASJC Scopus subject areas

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

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