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

被引：6

作者：

Jaikhan, Pattaporn ^{[1
]}

Buranrat, Benjaporn ^{[1
,2
]}

Itoh, Yukihiro ^{[1
]}

Chotitumnavee, Jiranan ^{[1
]}

Kurohara, Takashi ^{[1
]}

Suzuki, Takayoshi ^{[1
,3
]}

机构：

[1] Kyoto Prefectural Univ Med, Grad Sch Med Sci, Sakyo Ku, 1-5 Shimogamohangi Cho, Kyoto 6060823, Japan

[2] Mahasarakham Univ, Fac Med, Biomed Sci Res Unit, Muang Dist 44000, Maha Sarakham, Thailand

[3] Japan Sci & Technol Agcy JST, CREST, 4-1-8 Honcho, Kawaguchi, Saitama 3320012, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2019年 / 29卷 / 10期

关键词：

Small molecule; Drug design; Histone deacetylase; Lysine demethylase; Inhibitor; HISTONE DEMETHYLASES; CANCER; DOMAIN; METHYLATION; MECHANISMS;

D O I：

10.1016/j.bmcl.2019.03.028

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Fe(II)/alpha-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.

引用

页码：1173 / 1176

页数：4

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