Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist

…, R Rajapakse, VP Pathak, LC Christie…

文献索引：Li, Haitao; Anderes, Kenna L.; Kraynov, Eugenia A.; Luthin, David R.; Do, Quyen-Quyen; Hong, Yufeng; Tompkins, Eileen; Sun, Eric T.; Rajapakse, Ranjan; Pathak, Ved P.; Christie, Lance C.; Vazir, Haresh; Castillo, Rosemary; Gregory, Margaret L.; Castro, Mary; Nared-Hood, Karen; Paderes, Genevive; Anderson, Mark B. Journal of Medicinal Chemistry, 2006 , vol. 49, # 11 p. 3362 - 3367

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被引用次数: 10

摘要

Gonadotropin releasing hormone (GnRH) plays an important role in the biology of reproduction. The use of GnRH receptor antagonists has been reported in the literature for the treatment of breast, ovarian, and prostate cancers. In this article, we report the synthesis, in vitro characterization, pharmacokinetics, and pharmacodynamics of an orally bioavailable, potent, small molecule GnRH receptor antagonist N-{4, 6-dimethoxy-2-[(3- ...