Bioorganic & Medicinal Chemistry Letters 2009-05-15

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

Shohei Hamada, Tae-Dong Kim, Takayoshi Suzuki, Yukihiro Itoh, Hiroki Tsumoto, Hidehiko Nakagawa, Ralf Janknecht, Naoki Miyata

Index: Bioorg. Med. Chem. Lett. 19 , 2852-2855, (2009)

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Abstract

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.