27063-93-0Relevant articles and documents
Inhibition of the histone demethylase JMJD2E by 3-substituted pyridine 2,4-dicarboxylates
Thalhammer, Armin,Mecinovic, Jasmin,Loenarz, Christoph,Tumber, Anthony,Rose, Nathan R.,Heightman, Tom D.,Schofield, Christopher J.
scheme or table, p. 127 - 135 (2011/02/24)
Based on structural analysis of the human 2-oxoglutarate (2OG) dependent JMJD2 histone Nε-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 of a pyridine 2,4-dicarboxylate scaffold. The subsequently prepared di-acids were tested for in vitro inhibition of the histone demethylase JMJD2E and another human 2OG oxygenase, prolyl-hydroxylase domain isoform 2 (PHD2, EGLN1). A subset of substitution patterns yielded inhibitors with selectivity for JMJD2E over PHD2, demonstrating that structure-based inhibitor design can enable selective inhibition of histone demethylases over related human 2OG oxygenases.
Substituted pyridine-2,4-dicarboxylic acid derivatives and medicaments based on these compounds
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, (2008/06/13)
The invention relates to substituted pyridine-2,4-dicarboxylic acid derivatives of the formula I STR1 in which R1 and R2 have the meanings given. The invention also relates to a process for the preparation of the abovementioned compo
SUBSTITUTED ISOCYTOSINES HAVING HISTAMINE H2-ANTAGONIST ACTIVITY
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, (2008/06/13)
The compounds are substituted isocytosines which are histamine H 2-antagonists. Two specific compounds of the present inventon are 2-2-(5-methyl-4-imidazolylmethylthio)ethylamino!-5-(3-pyridylmethyl)-4-pyrimi done and 2-2-(3-bromo-2-pyridylmethylthio)ethylamino!-5-(4-pyridylmethyl)-4-pyrimidone .