The synthesis and bioactivity of the retinoid X receptor (RXR) antagonist 4-[(3'-n-butyl-5', 6', 7', 8'-tetrahydro-5', 5', 8', 8'-tetramethyl-2'-naphthalenyl)(cyclopropylidene) methyl] benzoic acid and several heteroatom-substituted analogues are described. Ligand design was based on the scaffold of the 3'-methyl RXR-selective agonist analogue and reports that 3'-n- propyl and longer n-alkyl groups conferred RXR antagonism. The transcriptional ...
