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

A Nakagawa, S Uno, M Makishima, H Miyachi…

文献索引：Nakagawa, Aya; Uno, Shigeyuki; Makishima, Makoto; Miyachi, Hiroyuki; Hashimoto, Yuichi Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 14 p. 7046 - 7054

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被引用次数: 12

摘要

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 74–78nM in alkaline phosphatase activity and reporter gene ...