242452-33-1Relevant articles and documents
The discovery of novel small molecule non-peptide gonadotropin releasing hormone (GnRH) receptor antagonists
Luthin, David R.,Hong, Yufeng,Pathak, Ved P.,Paderes, Genevieve,Nared-Hood, Karen D.,Castro, Mary A.,Vazir, Haresh,Li, Haitao,Tompkins, Eileen,Christie, Lance,May, John M.,Anderson, Mark B.
, p. 3467 - 3470 (2002)
A novel series of non-peptide derivatives 1, 14, and 15 that bind with high affinity to the human GnRH receptors is discussed. The discovery was made from screening our in-house libraries that contained the active structure 2 along with a trace amount of a second active structure 1 that was derived from an acid-induced rearrangement. From this structure type 1, a series of guanidine and non-guanidine containing analogues were prepared and tested as GnRH receptor antagonists. Compounds derived from this series bind to both human and rat GnRH receptors and antagonize GnRH-mediated increases in inositol phosphate production in cells containing recombinant human receptors. These compounds or their analogues may be useful as therapeutic agents for the treatment of hormone-dependent pathologies including prostate, breast and ovarian cancers.
Non-peptide GnRH agents, methods and intermediates for their preparation
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Page/Page column 14-15; 18-19, (2008/06/13)
Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.