Ontology highlight
ABSTRACT:
SUBMITTER: Li Z
PROVIDER: S-EPMC6663923 | biostudies-literature | 2019 Jul
REPOSITORIES: biostudies-literature
Li Zhonghua Z Ding Lina L Li Zhongrui Z Wang Zhizheng Z Suo Fengzhi F Shen Dandan D Zhao Taoqian T Sun Xudong X Wang Junwei J Liu Ying Y Ma Liying L Zhao Bing B Geng Pengfei P Yu Bin B Zheng Yichao Y Liu Hongmin H
Acta pharmaceutica Sinica. B 20190105 4
Histone lysine specific demethylase 1 (LSD1) has been recognized as an important modulator in post-translational process in epigenetics. Dysregulation of LSD1 has been implicated in the development of various cancers. Herein, we report the discovery of the hit compound <b>8a</b> (IC<sub>50</sub> = 3.93 μmol/L) and further medicinal chemistry efforts, leading to the generation of compound <b>15u</b> (IC<sub>50</sub> = 49 nmol/L, and <i>K</i> <sub>i</sub> = 16 nmol/L), which inhibited LSD1 reversi ...[more]