title: Aza-retinoids as novel retinoid X receptor-specific agonists.
abstract: 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.
authors.affiliation: Ligand Pharmaceuticals Inc., 10255 Science Center Drive, San Diego, CA 92121, USA. luc_farmer@vrtx.com
authors.forename: Luc J
authors.initials: LJ
authors.lastname: Farmer
authors.forename: Kristen S
authors.initials: KS
authors.lastname: Marron
authors.forename: Stacie S
authors.initials: SS
authors.lastname: Canan Koch
authors.forename: C K
authors.initials: CK
authors.lastname: Hwang
authors.forename: E Adam
authors.initials: EA
authors.lastname: Kallel
authors.forename: Lin
authors.initials: L
authors.lastname: Zhi
authors.forename: Alex M
authors.initials: AM
authors.lastname: Nadzan
authors.forename: Dave W
authors.initials: DW
authors.lastname: Robertson
authors.forename: Youssef L
authors.initials: YL
authors.lastname: Bennani
mesh_terms: 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
chemical_list: D001372:Aza Compounds; D047488:Retinoid X Receptors; D012176:Retinoids