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ID: ALA4392841

Journal: Bioorg Med Chem Lett

Title: Identification of ortho-hydroxy anilide as a novel scaffold for lysine demethylase 5 inhibitors.

Authors: Jaikhan P, Buranrat B, Itoh Y, Chotitumnavee J, Kurohara T, Suzuki T.

Abstract: Fe(II)/α-ketoglutarate-dependent lysine demethylases (KDMs) are attractive drug targets for several diseases including cancer. In this study, we designed and screened ortho-substituted anilides that are expected to function as Fe(II) chelators, and identified ortho-hydroxy anilide as a novel scaffold for KDM5A inhibitors. Treatment of human lung cancer A549 cells with a prodrug form of 4-carboxy-2-hydroxy-formanilide (9c) increased trimethylated lysine 4 on histone H3 level, suggesting KDM5 inhibition in the cells.

CiteXplore: 30928196

DOI: 10.1016/j.bmcl.2019.03.028