Aza-retinoids as novel retinoid X receptor-specific agonists.
A new structurally simple series of potent lipophilic aza-retinoids RXR agonists has been developed. SAR studies for the N-alkyl-azadienoic acids described here demonstrate that the RXR activity profile is sensitive to the N-alkyl chain length. Further, we have expanded the work to include azadienoic acids, which exhibited many accessible conformations leading to a better understanding of the SAR around the series.
Farmer
Luc J
LJ
Ligand Pharmaceuticals Inc., 10255 Science Center Drive, San Diego, CA 92121, USA. luc_farmer@vrtx.com
Marron
Kristen S
KS
Canan Koch
Stacie S
SS
Hwang
C K
CK
Kallel
E Adam
EA
Zhi
Lin
L
Nadzan
Alex M
AM
Robertson
Dave W
DW
Bennani
Youssef L
YL
D001372:Aza Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D047488:Retinoid X Receptors / Q000819:agonists*; D012176:Retinoids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D001372:Aza Compounds; D047488:Retinoid X Receptors; D012176:Retinoids