| Literature DB >> 15771412 |
Nicole C R van Straten1, Twan H J van Berkel, Dennis R Demont, Willem-Jan F Karstens, Remco Merkx, Julia Oosterom, Jürgen Schulz, Richard G van Someren, Cornelis M Timmers, Peter M van Zandvoort.
Abstract
Substituted 6-amino-4-phenyl-tetrahydroquinoline derivatives are described that are antagonists for the G(s)-protein-coupled human follicle-stimulating hormone (FSH) receptor. These compounds show high antagonistic efficacy in vitro using a CHO cell line expressing the human FSH receptor. Antagonist 10 also showed a submicromolar IC(50) in a more physiologically relevant rat granulosa cell assay and was found to significantly inhibit follicle growth and ovulation in an ex vivo mouse model. This compound class may open the way toward a novel, nonsteroidal approach for contraception.Entities:
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Year: 2005 PMID： 15771412 DOI： 10.1021/jm049676l
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446