Array synthesis of progesterone receptor antagonists: 3-Aryl-1,2-diazepines

New non-steroidal chemotypes are required for the development of drugs targeting the steroid hormone receptors. The parallel array synthesis of 3-aryl-1,2-diazepines employing solid-supported reagents is described. The resulting compounds demonstrated high affinity binding to the progesterone recept...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2006-07, Vol.16 (14), p.3777-3779
Hauptverfasser:	Wiethe, Robert W., Stewart, Eugene L., Drewry, David H., Gray, David W., Mehbob, Abdul, Hoekstra, William J.
Format:	Artikel
Sprache:	eng
Schlagworte:	Azepines - chemical synthesis Azepines - pharmacology Azirines - chemical synthesis Azirines - pharmacology Binding Sites Biological and medical sciences Cells, Cultured Diazepine Dihydropyridines - chemical synthesis Dihydropyridines - pharmacology Hormones. Endocrine system Humans Ligands Medical sciences Models, Chemical Pharmacology. Drug treatments Progesterone receptor Receptors, Progesterone - antagonists & inhibitors
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Beschreibung
Zusammenfassung:	New non-steroidal chemotypes are required for the development of drugs targeting the steroid hormone receptors. The parallel array synthesis of 3-aryl-1,2-diazepines employing solid-supported reagents is described. The resulting compounds demonstrated high affinity binding to the progesterone receptor.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2006.04.055