含有7-(5'-氰基吡咯-2-基)基团的1,5-二氢-苯并[e][1,4]恶唑嗪-2(1H)-酮作为非甾体孕酮受体调节剂。
1,5-Dihydro-benzo[e][1,4]oxazepin-2(1H)-ones containing a 7-(5'-cyanopyrrol-2-yl) group as nonsteroidal progesterone receptor modulators.
作者信息
Kern Jeffrey C, Terefenko Eugene A, Fensome Andrew, Unwalla Ray, Wrobel Jay, Cohen Jeffrey, Zhu Yuan, Berrodin Thomas J, Yudt Matthew R, Winneker Richard C, Zhang Zhiming, Zhang Puwen
机构信息
Chemical and Screening Sciences, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA.
出版信息
Bioorg Med Chem Lett. 2008 Sep 15;18(18):5015-7. doi: 10.1016/j.bmcl.2008.08.015. Epub 2008 Aug 9.
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.
制备了一系列新型的7-(5'-氰基吡咯-2-基)取代的苯并[1,4]恶唑-2-酮，并使用人T47D乳腺癌细胞系通过碱性磷酸酶测定法测试了它们的孕激素受体(PR)激动剂或拮抗剂活性。通过适当选择5-取代基，可同时获得PR激动剂和拮抗剂。几种类似物是有效的PR激动剂(如12和13)或PR拮抗剂(如18)，对其他甾体受体具有良好的选择性。
Zotero 插件