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DESIGN AND SYNTHESIS OF NOVEL RETINOID SYNERGISTS HAVING A DIBENZODIAZEPINE SKELETON

  作者 OHTA KIMINORI; KAWACHI EMIKO; SHUDO KOICHI; KAGECHIKA HIROYUKI  
  选自 期刊  Heterocycles;  卷期  2010年81-11;  页码  2465-2470  
  关联知识点  
 

[摘要]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.

 
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