Cell Penetrant Inhibitors Of The Kdm4 And Kdm5 Families Of Histone Lysine Demethylases. 2. Pyrido[3,4-D]Pyrimidin-4(3h)-One Derivatives
JOURNAL OF MEDICINAL CHEMISTRY(2016)
Abstract
Following the discovery of cell penetrant pyridine-4-carboxylate inhibitors of the KDM4 (JMJD2) and KDM5 (JARID1) families of histone lysine demethylases (e.g., 1), further optimization led to the identification of non-carboxylate inhibitors derived from pyrido[3,4-d]pyrimidin-4(3H)-one. A number of exemplars such as compound 41 possess interesting activity profiles in KDM4C and KDMSC biochemical and target-specific, cellular mechanistic assays.
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Key words
histone lysine demethylases,inhibitors,kdm4,kdm5 families
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