Development of the triazole-fused pyrimidine derivatives as highly potent and reversible inhibitors of histone lysine specific demethylase 1 (LSD1/KDM1A)

• Main Authors: Zhonghua Li (Author), Lina Ding (Author), Zhongrui Li (Author), Zhizheng Wang (Author), Fengzhi Suo (Author), Dandan Shen (Author), Taoqian Zhao (Author), Xudong Sun (Author), Junwei Wang (Author), Ying Liu (Author), Liying Ma (Author), Bing Zhao (Author), Pengfei Geng (Author), Bin Yu (Author), Yichao Zheng (Author), Hongmin Liu (Author)
• Format: Book
• Published: Elsevier, 2019-07-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

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 8a (IC50 = 3.93 μmol/L) and fu...