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

Robert W Wiethe; Eugene L Stewart; David H Drewry; David W Gray; Abdul Mehbob; William J Hoekstra

doi:10.1016/j.bmcl.2006.04.055

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

Bioorg Med Chem Lett. 2006 Jul 15;16(14):3777-9. doi: 10.1016/j.bmcl.2006.04.055. Epub 2006 May 5.

Authors

Robert W Wiethe¹, Eugene L Stewart, David H Drewry, David W Gray, Abdul Mehbob, William J Hoekstra

Affiliation

¹ Discovery Research, GlaxoSmithKline, Research Triangle Park, NC 27709-3398, USA.

PMID: 16678409
DOI: 10.1016/j.bmcl.2006.04.055

Abstract

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.

MeSH terms

Azepines / chemical synthesis*
Azepines / pharmacology*
Azirines / chemical synthesis
Azirines / pharmacology
Binding Sites
Cells, Cultured
Dihydropyridines / chemical synthesis
Dihydropyridines / pharmacology
Humans
Ligands
Models, Chemical
Receptors, Progesterone / antagonists & inhibitors*

Substances

Azepines
Azirines
Dihydropyridines
Ligands
Receptors, Progesterone
diazipine