Structure-Activity Relationship Study of N⁶-Benzoyladenine-Type BRD4 Inhibitors and Their Effects on Cell Differentiation and TNF-α Production

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  • Amemiya Seika
    Institute of Molecular & Cellular Biosciences, The University of Tokyo
  • Yamaguchi Takao
    Institute of Molecular & Cellular Biosciences, The University of Tokyo
  • Sakai Taki
    Institute of Molecular & Cellular Biosciences, The University of Tokyo
  • Hashimoto Yuichi
    Institute of Molecular & Cellular Biosciences, The University of Tokyo
  • Noguchi-Yachide Tomomi
    Institute of Molecular & Cellular Biosciences, The University of Tokyo

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  • Structure–Activity Relationship Study of <i>N</i><sup>6</sup>-Benzoyladenine-Type BRD4 Inhibitors and Their Effects on Cell Differentiation and TNF-α Production

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<p>Bromodomains are epigenetic ‘readers’ of histone acetylation. The first potent bromodomain and extra-terminal domain (BET) inhibitors, (+)-JQ1 and I-BET762 (also known as GSK525762), were reported in 2010. Some BET inhibitors are already under clinical trial for the treatment of cancers, but so far, only a few chemical scaffolds are available. We have reported potent N6-benzoyladenine-based inhibitors of BRD4, a BET family member that serves as a key mediator of transcriptional elongation. Here we present an analysis of the structure–activity relationships of these inhibitors. Among the compounds examined, 20, 28 and 29 enhanced all-trans retinoic acid (ATRA)-induced HL-60 cell differentiation and inhibited tumor necrosis factor (TNF)-α production by THP-1 cells.</p>

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