Synthesis and activity of N-oxalylglycine and its derivatives as Jumonji C-domain-containing histone lysine demethylase inhibitors

N-Oxalylglycine (NOG) derivatives were synthesized, and their inhibitory effect on histone lysine demethylase activity was evaluated. NOG and compound 1 inhibited histone lysine demethylases JMJD2A, 2C and 2D in enzyme assays, and their dimethyl ester prodrugs DMOG and 21 exerted histone lysine methylating activity in cellular assays.

N-Oxalylglycine (NOG) derivatives were synthesized and their inhibitory effect on histone lysine demethylase activity was evaluated. This study showed that NOG and compound 1 inhibit histone lysine demethylases both in enzyme assays and cellular assays.Figure optionsDownload as PowerPoint slide