Progesterone receptor antagonists with a 3-phenylquinazoline-2,4-dione/2-phenylisoquinoline-1,3-dione skeleton.
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 IC(50) values of 74-78nM in alkaline phosphatase activity and reporter gene assays.
Nakagawa
Aya
A
Institute of Molecular & Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan. Aya.Nakagawa@mitsui-chem.co.jp
Uno
Shigeyuki
S
Makishima
Makoto
M
Miyachi
Hiroyuki
H
Hashimoto
Yuichi
Y
D000469:Alkaline Phosphatase; D000818:Animals; D016466:CHO Cells; D045744:Cell Line, Tumor; D006224:Cricetinae; D003412:Cricetulus; D017930:Genes, Reporter; D006801:Humans; D020128:Inhibitory Concentration 50; D011799:Quinazolines / Q000737:chemistry / Q000494:pharmacology*; D011804:Quinolines / Q000737:chemistry / Q000494:pharmacology*; D011980:Receptors, Progesterone / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D011799:Quinazolines; D011804:Quinolines; D011980:Receptors, Progesterone; D000469:Alkaline Phosphatase