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Updated: Aug 8, 2026

In Vitro Imaging and Quantification of the Drug Targeting Efficiency of Fluorescently Labeled GnRH Analogues
Published on: March 21, 2017
Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist
Haitao Li1, Kenna L Anderes, Eugenia A Kraynov
1Department of Medicinal Chemistry, Research Pharmacology, and Pharmacokenetics, Dynamics & Metabolism, Pfizer Global Research & Development, 10770 Science Center Drive, San Diego, California 92121, USA. haitao.li@pfizer.com
Abstract:
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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