title: 1,5-Dihydro-benzo[e][1,4]oxazepin-2(1H)-ones containing a 7-(5'-cyanopyrrol-2-yl) group as nonsteroidal progesterone receptor modulators.
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.
authors: Chemical and Screening Sciences, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA.
authors: Jeffrey C
authors: JC
authors: Kern
authors: Eugene A
authors: EA
authors: Terefenko
authors: Andrew
authors: A
authors: Fensome
authors: Ray
authors: R
authors: Unwalla
authors: Jay
authors: J
authors: Wrobel
authors: Jeffrey
authors: J
authors: Cohen
authors: Yuan
authors: Y
authors: Zhu
authors: Thomas J
authors: TJ
authors: Berrodin
authors: Matthew R
authors: MR
authors: Yudt
authors: Richard C
authors: RC
authors: Winneker
authors: Zhiming
authors: Z
authors: Zhang
authors: Puwen
authors: P
authors: Zhang
mesh_terms: D020650:Combinatorial Chemistry Techniques; D006801:Humans; D015394:Molecular Structure; D010077:Oxazepines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011980:Receptors, Progesterone / Q000819:agonists* / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D010077:Oxazepines; D011980:Receptors, Progesterone