SAR studies of 6-(arylamino)-4, 4-disubstituted-1-methyl-1, 4-dihydro-benzo [d][1, 3] oxazin-2-ones as progesterone receptor antagonists

…, Y Zhu, J Cohen, R Winneker, Z Zhang, P Zhang

Index: Kern, Jeffrey C.; Terefenko, Eugene A.; Fensome, Andrew; Unwallla, Ray; Wrobel, Jay; Zhu, Yuan; Cohen, Jeffrey; Winneker, Richard; Zhang, Zhiming; Zhang, Puwen Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 1 p. 189 - 192

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Citation Number: 35

Abstract

We previously disclosed that 6-aryl benzoxazin-2-ones were PR modulators. In a continuation of this work we examined the SAR of new 6-arylamino benzoxazinones and found the targets 1–25, with an extra amino linker between the pendent 6-aryl groups and benzoxazinone or benzoxazine-2-thione core, were PR antagonists. A series of compounds with substituents at the 1-and 4-positions as well as different 6-aryl groups were prepared ...