Title of article
Progesterone receptor antagonists with a 3-phenylquinazoline-2,4-dione/2-phenylisoquinoline-1,3-dione skeleton Original Research Article
Author/Authors
Aya Nakagawa، نويسنده , , Shigeyuki Uno، نويسنده , , Makoto Makishima، نويسنده , , Hiroyuki Miyachi، نويسنده , , Yuichi Hashimoto، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
9
From page
7046
To page
7054
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.
Keywords
Progesterone , Antagonist , isoquinoline , Nuclear receptor ligand , Structural development
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2008
Journal title
Bioorganic and Medicinal Chemistry
Record number
1306750
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