期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 59, 期 4, 页码 1357-1369出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.5b01537
关键词
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Optimization of KDM6B (JMJD3) HTS hit 12 led to the identification of 3-((furan-2-ylmethyl)amino)pyridine-4-carboxylic acid 34 and 3-(((3-methylthiophen-2-yl)methyl)amino)pyridine-4-carboxylic acid 39 that are inhibitors of the KDM4 (JMJD2) family of histone lysine demethylases. Compounds 34 and 39 possess activity, IC50 <= 100 nM, in KDM4 family biochemical (RFMS) assays with >= 50-fold selectivity against KDM6B and activity in a mechanistic KDM4C cell imaging assay (IC50 = 6-8 mu M). Compounds 34 and 39 are also potent inhibitors of KDM5C (JARID1C) (RFMS IC50 = 100-125 nM).
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