| Autor: |
Li H; 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, Anderes KL, Kraynov EA, Luthin DR, Do QQ, Hong Y, Tompkins E, Sun ET, Rajapakse R, Pathak VP, Christie LC, Feng J, Vazir H, Castillo R, Gregory ML, Castro M, Nared-Hood K, Paderes G, Anderson MB |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of medicinal chemistry [J Med Chem] 2006 Jun 01; Vol. 49 (11), pp. 3362-7. |
| DOI: |
10.1021/jm060012g |
| Abstrakt: |
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). |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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