1992-01-4Relevant articles and documents
Novel Nonsteroidal Progesterone Receptor (PR) Antagonists with a Phenanthridinone Skeleton
Nishiyama, Yuko,Mori, Shuichi,Makishima, Makoto,Fujii, Shinya,Kagechika, Hiroyuki,Hashimoto, Yuichi,Ishikawa, Minoru
supporting information, p. 641 - 645 (2018/07/05)
The progesterone receptor (PR) plays an important role in various physiological systems, including female reproduction and the central nervous system, and PR antagonists are thought to be effective not only as contraceptive agents and abortifacients but also in the treatment of various diseases, including hormone-dependent cancers and endometriosis. Here, we identified phenanthridin-6(5H)-one derivatives as a new class of PR antagonists and investigated their structure-activity relationships. Among the synthesized compounds, 37, 40, and 46 exhibited very potent PR antagonistic activity with high selectivity for PR over other nuclear receptors. These compounds are structurally distinct from other nonsteroidal PR antagonists, including cyanoaryl derivatives, and should be useful for further studies of the clinical utility of PR antagonists.
Liver X receptor (LXR) modulators with dibenz[b,f]-[1,4]oxazepin-11-one, (Z)-dibenz[b,f]azocin-6-one, and 11,12-dihydrodibenz[b,f]azocin-6-one skeletons
Aoyama, Atsushi,Aoyama, Hiroshi,Makishima, Makoto,Hashimoto, Yuichi,Miyachi, Hiroyuki
scheme or table, p. 2209 - 2216 (2010/04/29)
Conformationally restricted heterocyclic analogs of carba-T0901317 with dibenz[b,f][1,4]oxazepin-11-one, 11,12-dihydrodibenz[b,f)azocin-6-one, and (Z)-dibenz[b,f]-azocin-6-one skeletons were prepared as candidate for liver X receptor (LXR) agonists. In vitro transactivation assay revealed that the activity depends on the nature of the linking group.
Antihypertensive polyfluorohydroxyisopropyl bicyclic and tricyclic carbostyrils
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, (2008/06/13)
Polyfluorohydroxyisopropyl bicyclic and tricyclic carbostyrils, such as 2,3-dihydro-7-methyl-9-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]-5H-pyrido[1,2,3-de]-1,4-benzoxazin-5-one, useful as antihypertensive agents.