Discovery of a Novel, Orally Active, Small Molecule Gonadotropin-Releasing Hormone (GnRH) Receptor Antagonist

Department of Medicinal Chemistry, Research Pharmacology, and Pharmacokenetics, Dynamics & Metabolism, Pfizer Global Research & Development, 10770 Science Center Drive, San Diego, California 92121, USA.
Journal of Medicinal Chemistry (Impact Factor: 5.45). 07/2006; 49(11):3362-7. DOI: 10.1021/jm060012g
Source: PubMed


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-morpholin-4-ylpropyl)amino]pyrimidin-5-yl}-5-[3,3,6-trimthyl-2,3-dihydro-1H-inden-5-yl)oxy]-2-furamide (compound 1).

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