Design, synthesis and SAR of uracil diamines as potent GnRH receptor antagonists

MEDI 81

Charles Huang, chuang@neurocrine.com1, Warren Wade1, Yun-Fei Zhu1, Chen Chen1, Zack Guo1, Yongsheng Chen1, Scott Struthers2, Martin W. Rowbottom, mrowbottom@neurocrine.com1, Jamie Rueter1, Duncan Wu1, Joann Xie2, and John Saunders1. (1) Department of Medicinal Chemistry, Neurocrine Biosciences Inc, 12790 El Camino Real, San Diego, CA 92130, (2) Department of Endocrinology, Neurocrine Biosciences Inc, 12790 El Camino Real, San Diego, CA 92130
Gonadotropin-releasing hormone (GnRH), or luteinizing hormone-releasing hormone (LHRH) is believed to play a very important role in modulating reproductive functions. Non-peptide GnRH antagonists have been extensively studied due to their potential therapeutic benefit in treating endometriosis, uterine fibroids, and prostate and breast cancers. A series of uracil diamines were discovered as novel and potent GnRH receptor antagonists. Chemical synthesis and structure-activity relationship (SAR) of this series will be presented.
 

Poster Session
7:00 PM-9:00 PM, Sunday, August 19, 2007 BCEC -- Exhibit Hall - B2, Poster

Division of Medicinal Chemistry

The 234th ACS National Meeting, Boston, MA, August 19-23, 2007