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

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.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2007-08, Vol.17 (15), p.4158-4162
Hauptverfasser:	ARDECKY, Robert J, HUDSON, Andrew R, LOPEZ, Francisco J, MARSCHKE, Keith B, MINER, Jeffrey N, KARANEWSKY, Donald S, NEGRO-VILAR, Andrés, LIN ZHI, PHILLIPS, Dean P, TYHONAS, John S, DECKHUT, Charlotte, LAU, Thomas L, YONGKAI LI, MARTINBOROUGH, Esther A, ROACH, Steven L, HIGUCHI, Robert I
Format:	Artikel
Sprache:	eng
Schlagworte:	Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Chrysenes - chemical synthesis Chrysenes - chemistry Chrysenes - pharmacology Hormones. Endocrine system Medical sciences Pharmacology. Drug treatments Receptors, Glucocorticoid - drug effects Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2007.05.062