Synthesis and biological evaluation of piperazinyl heterocyclic antagonists of the gonadotropin releasing hormone (GnRH) receptor

…, DB Hauze, CW Mann, JF Mehlmann, JF Rogers…

文献索引：Vera, Matthew D.; Lundquist IV, Joseph T.; Chengalvala, Murty V.; Cottom, Joshua E.; Feingold, Irene B.; Garrick, Lloyd M.; Green, Daniel M.; Hauze, Diane B.; Mann, Charles W.; Mehlmann, John F.; Rogers, John F.; Shanno, Linda; Wrobel, Jay E.; Pelletier, Jeffrey C. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 8 p. 2512 - 2515

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被引用次数: 3

摘要

Antagonism of the gonadotropin releasing hormone (GnRH) receptor has resulted in positive clinical results in reproductive tissue disorders such as endometriosis and prostate cancer. Following the recent discovery of orally active GnRH antagonists based on a 4- piperazinylbenzimidazole template, we sought to investigate the properties of heterocyclic isosteres of the benzimidazole template. We report here the synthesis and biological ...