Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3, 3-dimethyl-2-oxo-2, 3-dihydro-1 H-indol-5-yl)-1-methyl …

…, J Cohen, C Huselton, A Illenberger…

文献索引：Fensome, Andrew; Adams, William R.; Adams, Andrea L.; Berrodin, Tom J.; Cohen, Jeff; Huselton, Christine; Illenberger, Arthur; Kern, Jeffrey C.; Hudak, Valerie A.; Marella, Michael A.; Melenski, Edward G.; McComas, Casey C.; Mugford, Cheryl A.; Slayden, Ov D.; Yudt, Matthew; Zhang, Zhiming; Zhang, Puwen; Zhu, Yuan; Winneker, Richard C.; Wrobel, Jay E. Journal of Medicinal Chemistry, 2008 , vol. 51, # 6 p. 1861 - 1873

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被引用次数: 123

摘要

We have continued to explore the 3, 3-dialkyl-5-aryloxindole series of progesterone receptor (PR) modulators looking for new agents to be used in female healthcare: contraception, fibroids, endometriosis, and certain breast cancers. Previously we reported that subtle structural changes with this and related templates produced functional switches between agonist and antagonist properties (Fensome et al. Biorg. Med. Chem. Lett. 2002, 12, 3487; ...