6-Aryl-1, 4-dihydro-benzo [d][1, 3] oxazin-2-ones: a novel class of potent, selective, and orally active nonsteroidal progesterone receptor antagonists

P Zhang, EA Terefenko, A Fensome…

Index: Zhang, Puwen; Terefenko, Eugene A.; Fensome, Andrew; Wrobel, Jay; Winneker, Richard; Lundeen, Scott; Marschke, Keith B.; Zhang, Zhiming Journal of Medicinal Chemistry, 2002 , vol. 45, # 20 p. 4379 - 4382

Full Text: HTML

Citation Number: 67

Abstract

Novel 6-aryl-1, 4-dihydro-benzo [d][1, 3] oxazin-2-ones were synthesized and tested as progesterone receptor (PR) antagonists. These compounds were potent and showed good selectivity for PR over other steroid receptors such as the glucocorticoid and androgen receptors (eg, greater than 80-fold selectivity at PR for 4h). Numerous 6-aryl benzoxazinones (eg, 4h-j) were active orally in the uterine decidualization and component ...