title: Diarylamines incorporating hexahydrophenalene or octahydrobenzoheptalene as retinoid X receptor (RXR)-specific agonists.
abstract: Selective ligands for retinoic acid receptors (RARs) and for retinoid X receptors (RXRs) are required for both biological studies and therapeutic purposes. We have synthesized a series of diarylamines incorporating hexahydrophenalene or octahydrobenzoheptalene as a hydrophobic moiety and examined their activities towards RARs and RXRs. Most of these compounds showed agonistic activity towards RXRs, but were inactive towards RARs. These RXR-specific ligands showed synergistic activity in RARα,β ligand-induced terminal differentiation of leukemia cell line HL-60.
authors.affiliation: Research Foundation ITSUU Laboratory.
authors.forename: Yohei
authors.initials: Y
authors.lastname: Amano
authors.forename: Masayuki
authors.initials: M
authors.lastname: Noguchi
authors.forename: Koichi
authors.initials: K
authors.lastname: Shudo
mesh_terms: D000588:Amines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000818:Animals; D001567:Benzocycloheptenes / Q000737:chemistry; D019556:COS Cells; D002454:Cell Differentiation / Q000187:drug effects; D002522:Chlorocebus aethiops; D004357:Drug Synergism; D018922:HL-60 Cells; D006801:Humans; D043803:Phenalenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D047488:Retinoid X Receptors / Q000819:agonists*; D013329:Structure-Activity Relationship
chemical_list: D000588:Amines; D001567:Benzocycloheptenes; D043803:Phenalenes; D047488:Retinoid X Receptors