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.
Ardecky
Robert J
RJ
Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive, San Diego, CA 92121, USA.
Hudson
Andrew R
AR
Phillips
Dean P
DP
Tyhonas
John S
JS
Deckhut
Charlotte
C
Lau
Thomas L
TL
Li
Yongkai
Y
Martinborough
Esther A
EA
Roach
Steven L
SL
Higuchi
Robert I
RI
Lopez
Francisco J
FJ
Marschke
Keith B
KB
Miner
Jeffrey N
JN
Karanewsky
Donald S
DS
Negro-Vilar
Andrés
A
Zhi
Lin
L
D002911:Chrysenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011965:Receptors, Glucocorticoid / Q000187:drug effects*; D013329:Structure-Activity Relationship
D002911:Chrysenes; D011965:Receptors, Glucocorticoid; C031180:chrysene