Literature DB >> 16722655

Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist.

Haitao Li1, Kenna L Anderes, Eugenia A Kraynov, David R Luthin, Quyen-Quyen Do, Yufeng Hong, Eileen Tompkins, Eric T Sun, Ranjan Rajapakse, Ved P Pathak, Lance C Christie, Jun Feng, Haresh Vazir, Rosemary Castillo, Margaret L Gregory, Mary Castro, Karen Nared-Hood, Genevieve Paderes, Mark B Anderson.   

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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Year:  2006        PMID: 16722655     DOI: 10.1021/jm060012g

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  1 in total

Review 1.  Recent Development of Non-Peptide GnRH Antagonists.

Authors:  Feng-Ling Tukun; Dag Erlend Olberg; Patrick J Riss; Ira Haraldsen; Anita Kaass; Jo Klaveness
Journal:  Molecules       Date:  2017-12-09       Impact factor: 4.411

  1 in total

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