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J Med Chem. 2006 Jun 1;49(11):3362-7.

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

Author information

1
Department 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

Erratum in

  • J Med Chem. 2006 Sep 21;49(19):5849. Feng, Jun [added].

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).

PMID:
16722655
DOI:
10.1021/jm060012g
[Indexed for MEDLINE]

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