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

…, WJF Karstens, R Merkx, J Oosterom…

Index: Van Straten, Nicole C. R.; Van Berkel, Twan H. J.; Demont, Dennis R.; Karstens, Willem-Jan F.; Merkx, Remco; Oosterom, Julia; Schulz, Juergen; Van Someren, Richard G.; Timmers, Cornelis M.; Van Zandvoort, Peter M. Journal of Medicinal Chemistry, 2005 , vol. 48, # 6 p. 1697 - 1700

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Citation Number: 66

Abstract

Substituted 6-amino-4-phenyl-tetrahydroquinoline derivatives are described that are antagonists for the Gs-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 IC50 in a more physiologically relevant rat granulosa cell assay and was found to significantly inhibit ...