Synthesis and Structure–Activity Relationship Study of Triazine-Based Inhibitors of the DNA Binding of NF-κB

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  • Fujii Shinya
    Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University Institute of Molecular and Cellular Biosciences, The University of Tokyo
  • Kobayashi Takanobu
    Kagawa School of Pharmaceutical Sciences, Tokushima Bunri University
  • Nakatsu Aki
    Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University
  • Miyazawa Hiroshi
    Kagawa School of Pharmaceutical Sciences, Tokushima Bunri University
  • Kagechika Hiroyuki
    Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University

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Nuclear transcription factor nuclear factor-kappa B (NF-κB) has diverse pathophysiological functions, and NF-κB inhibitors are considered to be candidates for multiple therapeutic applications. We previously reported a novel triazine-based NF-κB inhibitor, 2-anilino-4,6-dichloro-1,3,5-triazine (NI241), that directly inhibits DNA binding of NF-κB. Here, we report synthesis of a series of triazine derivatives and evaluation of their structure–activity relationships for NF-κB inhibition. We found that 2-amino-4,6-dichloro-1,3,5-triazine substructure is essential for the inhibitory activity of the lead compound NI241, and modification of NI241 by introduction of an m-methoxy substituent on the phenyl ring afforded the more potent derivative 28. The structure–activity relationships identified in this study suggested a possible mechanism of irreversible NF-κB inhibition by NI241, and should be helpful in the design of other NF-κB inhibitors.

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