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■ Synthesis of LSD1 Inhibitor-Pyrrole-Imidazole Polyamide Conjugates for Region-Specific Alterations of Histone Modification

Rui Qin, Shihori Takayanagi, Yusuke Kondo, Jiawei Li, Naoki Shiga, Masaya Nakajima, Ken-ichi Shinohara, Natsumi Yoda, Takayoshi Suzuki, Atsushi Kaneda, and Tetsuhiro Nemoto*

*Graduate School of Pharmaceutical Sciences, Chiba University, 1-8-1, Inohana, Chuo-ku, Chiba 260-8675, Japan

Abstract

Synthetic method of LSD1 inhibitor–pyrrole-imidazole polyamide conjugates for region specific alterations of histone modification is described. A (1S,2R)-tranylcypromine (PCPA) unit was coupled with an L-lysine part using a nosyl strategy. Conjugation of the inhibitor part with PIP tetramer units was achieved by amide bond formation using PyBOP as a condensation reagent.