Tomoya Hirano, Takashi Fujiwara, Hideaki Niwa, Michitake Hirano, Kasumi Ohira, Yusuke Okazaki, Shin Sato, Takashi Umehara, Yuki Maemoto, Akihiro Ito, Minoru Yoshida, Hiroyuki Kagechika
The histone methyltransferase SET7/9 methylates not only histone but also non-histone proteins as substrates, and therefore, SET7/9 inhibitors are considered candidates for the treatment of diseases. Previously, our group identified cyproheptadine, used clinically as a serotonin receptor antagonist and histamine receptor (H1) antagonist, as a novel scaffold of the SET7/9 inhibitor. In this work, we focused on dibenzosuberene as a substructure of cyproheptadine and synthesized derivatives with various functional groups...
August 10, 2018: ChemMedChem