Title of article :
1,5-Dihydro-benzo[e][1,4]oxazepin-2(1H)-ones containing a 7-(5′-cyanopyrrol-2-yl) group as nonsteroidal progesterone receptor modulators
Author/Authors :
Jeffrey C. Kern، نويسنده , , Eugene A. Terefenko، نويسنده , , Andrew Fensome، نويسنده , , Ray Unwalla، نويسنده , , Jay Wrobel، نويسنده , , Jeffrey Cohen، نويسنده , , Yuan Zhu، نويسنده , , Thomas J. Berrodin، نويسنده , , Matthew R. Yudt، نويسنده , , Richard C. Winneker، نويسنده , , Zhiming Zhang، نويسنده , , Puwen Zhang، نويسنده ,
Abstract :
A series of novel 7-(5′-cyanopyrrol-2-yl) substituted benzo[1,4]oxazepin-2-ones were prepared and tested for their progesterone receptor (PR) agonist or antagonist activity in the alkaline phosphatase assay using the human T47D breast carcinoma cell line. Both PR agonists and antagonists were achieved with an appropriate choice of 5-substitution. Several analogs were potent PR agonists (e.g., 12 and 13) or PR antagonists (e.g., 18) with good selectivity over other steroid receptors.
Keywords :
non-steroidal , Progesterone receptor (PR) , PR antagonist , PR agonist
