876162-62-8Relevant articles and documents
Identification of ortho-hydroxy anilide as a novel scaffold for lysine demethylase 5 inhibitors
Jaikhan, Pattaporn,Buranrat, Benjaporn,Itoh, Yukihiro,Chotitumnavee, Jiranan,Kurohara, Takashi,Suzuki, Takayoshi
, p. 1173 - 1176 (2019/03/29)
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.