865670-11-7Relevant articles and documents
7-Aryl 1,5-dihydro-benzo[e][1,4]oxazepin-2-ones and analogs as non-steroidal progesterone receptor antagonists
Zhang, Puwen,Kern, Jeffrey C.,Terefenko, Eugene A.,Fensome, Andrew,Unwalla, Ray,Zhang, Zhiming,Cohen, Jeffrey,Berrodin, Thomas J.,Yudt, Matthew R.,Winneker, Richard C.,Wrobel, Jay
, p. 6589 - 6600 (2008/12/21)
Novel 7-aryl benzo[1,4]oxazepin-2-ones were synthesized and evaluated as non-steroidal progesterone receptor (PR) modulators. The structure activity relationship of 7-aryl benzo[1,4]oxazepinones was examined using the T47D cell alkaline phosphatase assay. A number of 7-aryl benzo[1,4]oxazepinones such as 10j and 10v demonstrated good in vitro potency (IC50 of 10-30 nM) and selectivity (over 100-fold) at PR over other steroidal receptors such as glucocorticoid and androgen receptors (GR and AR). Several 7-aryl benzo[1,4]oxazepinones were active in the rat uterine decidualization model. In this in vivo model, compounds 10j and 10u were active at 3 mg/kg when dosed orally.