DESIGN AND SYNTHESIS OF NOVEL RETINOID SYNERGISTS HAVING A DIBENZODIAZEPINE SKELETON

Based on the structures of potent RXR agonists 2 and 3, novel dibenzodiazepine derivatives 4 ― 6, containing two diphenylamine substructures, were designed as RXR modulator candidates and synthesized by utilizing Pd-catalyzed and Cu-promoted diphenylamine-generating reactions as key reactions. These compounds showed retinoid-synergistic activity, enhancing the HL-60 cell differentiation-inducing ability of the RAR agonist Am80.