Potent nonsteroidal progesterone receptor agonists: synthesis and SAR study of 6-aryl benzoxazines.
作者： Puwen Zhang , Eugene A. Terefenko , Andrew Fensome , Zhiming Zhang , Yuan Zhu
DOI: 10.1016/S0960-894X(02)00025-2
关键词:
摘要: Abstract Novel 6-aryl benzoxazines were prepared and examined as progesterone receptor (PR) modulators. In contrast to the structurally related dihydroquinoline PR antagonists, potent agonists. Compounds 4e, 5b, 6a with 2,4,4-trimethyl-1,4-dihydro-2H-benzo[d][1,3]oxazine core most agonists in series sub-nanomolar activities (EC50 0.20–0.35 nM). Compound was more than (P4) vivo decidualization assay an ovariectomized female rat model by subcutaneous administration ED50 of 1.5 mg/kg (vs 5.62 mg/kg for P4).
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