Progesterone receptor antagonists with a 3-phenylquinazoline-2,4-dione/2-phenylisoquinoline-1,3-dione skeleton

Aya Nakagawa, Shigeyuki Uno, Makoto Makishima, Hiroyuki Miyachi, Yuichi Hashimoto

Research output: Contribution to journalArticle

13 Citations (Scopus)

Abstract

Novel non-steroidal progesterone receptor antagonists with a 3-phenylquinazoline-2,4-dione/2-phenylisoquinoline-1,3-dione skeleton were developed and their structure-activity relationships were investigated. Among the prepared compounds, 4-(4,4-diethyl-3,4-dihydro-1,3-dioxoquinolin-2(1H)-yl)benzonitrile (DEPIQ-4CN) showed the most potent activity, with IC50 values of 74-78 nM in alkaline phosphatase activity and reporter gene assays.

Original languageEnglish
Pages (from-to)7046-7054
Number of pages9
JournalBioorganic and Medicinal Chemistry
Volume16
Issue number14
DOIs
Publication statusPublished - Jul 15 2008
Externally publishedYes

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Keywords

  • Antagonist
  • Isoquinoline
  • Nuclear receptor ligand
  • Progesterone
  • Structural development

ASJC Scopus subject areas

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

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