2. Academic Validation
  3. Identification of substituted 6-amino-4-phenyltetrahydroquinoline derivatives: potent antagonists for the follicle-stimulating hormone receptor

Identification of substituted 6-amino-4-phenyltetrahydroquinoline derivatives: potent antagonists for the follicle-stimulating hormone receptor

  • J Med Chem. 2005 Mar 24;48(6):1697-700. doi: 10.1021/jm049676l.
Nicole C R van Straten 1,  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
Affiliations

Affiliation

  • 1 Lead Discovery Unit, Research and Development, N.V. Organon, P.O. Box 20, 5340 BH Oss, The Netherlands. nicole.vanstraten@organon.com
PMID: 15771412 DOI: 10.1021/jm049676l
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.

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