Synthesis of orally active small-molecule gonadotropin-releasing hormone antagonists.
Recent success in the search for orally active gonadotropin-releasing hormone antagonists for the treatment of sex hormone-related diseases, such as endometriosis, uterine fibroids and prostate cancer, has resulted in the discovery of non-peptide compounds from several different chemical classes. At least two such compounds have advanced to the clinic for testing in humans, while multiple series of compounds have demonstrated oral activity in animal studies. This review covers the basic biological activity and the syntheses of these compounds, focusing on progress made over the past year.
Tucci
Fabio C
FC
Neurocrine Biosciences Inc, San Diego, CA 92130, USA.
Chen
Chen
C
D000284:Administration, Oral; D000818:Animals; D007987:Gonadotropin-Releasing Hormone / Q000037:antagonists & inhibitors*; D006727:Hormone Antagonists / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D007202:Indicators and Reagents
D006727:Hormone Antagonists; D007202:Indicators and Reagents; D007987:Gonadotropin-Releasing Hormone