Inhibition of the histone demethylase JMJD2E by 3-substituted pyridine 2, 4-dicarboxylates

…, NR Rose, TD Heightman, CJ Schofield

Index: Thalhammer, Armin; Mecinovic, Jasmin; Loenarz, Christoph; Tumber, Anthony; Rose, Nathan R.; Heightman, Tom D.; Schofield, Christopher J. Organic and Biomolecular Chemistry, 2011 , vol. 9, # 1 p. 127 - 135

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Citation Number: 30

Abstract

Based on structural analysis of the human 2-oxoglutarate (2OG) dependent JMJD2 histoneNε-methyl lysyl demethylase family, 3-substituted pyridine 2, 4-dicarboxylic acids were identified as potential inhibitors with possible selectivity over other human 2OG oxygenases. Microwave-assisted palladium-catalysed cross coupling methodology was developed to install a diverse set of substituents on the sterically demanding C-3 position ...