5(Z)-benzylidene-1,2-dihydro-9-hydroxy-10-methoxy-2,2,4-trimethyl-5H-1-aza-6-oxa-chrysenes as non-steroidal glucocorticoid receptor modulators.

5(Z)-benzylidene-1,2-dihydro-9-hydroxy-10-methoxy-2,2,4-trimethyl-5H-1-aza-6-oxa-chrysenes as non-steroidal glucocorticoid receptor modulators.

Bioorganic & medicinal chemistry letters (2007-06-08)

Robert J Ardecky, Andrew R Hudson, Dean P Phillips, John S Tyhonas, Charlotte Deckhut, Thomas L Lau, Yongkai Li, Esther A Martinborough, Steven L Roach, Robert I Higuchi, Francisco J Lopez, Keith B Marschke, Jeffrey N Miner, Donald S Karanewsky, Andrés Negro-Vilar, Lin Zhi

PMID17553679

摘要

A series of 5-benzylidene-1,2-dihydro-2,2,4-trimethyl-5H-1-aza-6-oxa-chrysenes was synthesized and profiled for their ability to act as selective glucocorticoid receptor modulators (SGRMs). The synthesis and structure-activity relationships for this series of compounds are presented.