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. 2002 Mar 11;12(5):787-90.
doi: 10.1016/s0960-894x(02)00025-2.

Potent nonsteroidal progesterone receptor agonists: synthesis and SAR study of 6-aryl benzoxazines

Puwen Zhang  1 , Eugene A Terefenko, Andrew Fensome, Zhiming Zhang, Yuan Zhu, Jeffrey Cohen, Richard Winneker, Jay Wrobel, John Yardley
Affiliations

Potent nonsteroidal progesterone receptor agonists: synthesis and SAR study of 6-aryl benzoxazines

Puwen Zhang et al. Bioorg Med Chem Lett. .

Abstract

Novel 6-aryl benzoxazines were prepared and examined as progesterone receptor (PR) modulators. In contrast to the structurally related 6-aryl dihydroquinoline PR antagonists, the 6-aryl benzoxazines were potent PR agonists. Compounds 4e, 5b, and 6a with the 2,4,4-trimethyl-1,4-dihydro-2H-benzo[d][1,3]oxazine core were the most potent PR agonists in the series with sub-nanomolar activities (EC(50) 0.20-0.35nM). Compound 6a was more potent than progesterone (P4) in the in vivo decidualization assay in an ovariectomized female rat model by subcutaneous administration with an ED(50) of 1.5mg/kg (vs 5.62mg/kg for P4).

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