2. Academic Validation
  3. 1,5-Dihydro-benzo[e][1,4]oxazepin-2(1H)-ones containing a 7-(5'-cyanopyrrol-2-yl) group as nonsteroidal progesterone receptor modulators

1,5-Dihydro-benzo[e][1,4]oxazepin-2(1H)-ones containing a 7-(5'-cyanopyrrol-2-yl) group as nonsteroidal progesterone receptor modulators

  • Bioorg Med Chem Lett. 2008 Sep 15;18(18):5015-7. doi: 10.1016/j.bmcl.2008.08.015.
Jeffrey C Kern 1,  Eugene A Terefenko,  Andrew Fensome,  Ray Unwalla,  Jay Wrobel,  Jeffrey Cohen,  Yuan Zhu,  Thomas J Berrodin,  Matthew R Yudt,  Richard C Winneker,  Zhiming Zhang,  Puwen Zhang
Affiliations

Affiliation

  • 1 Chemical and Screening Sciences, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA.
PMID: 18722119 DOI: 10.1016/j.bmcl.2008.08.015
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.

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