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

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 (IC(50) = 3.93 μmol/L) and...

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Gepubliceerd in:Acta Pharm Sin B
Hoofdauteurs: Li, Zhonghua, Ding, Lina, Li, Zhongrui, Wang, Zhizheng, Suo, Fengzhi, Shen, Dandan, Zhao, Taoqian, Sun, Xudong, Wang, Junwei, Liu, Ying, Ma, Liying, Zhao, Bing, Geng, Pengfei, Yu, Bin, Zheng, Yichao, Liu, Hongmin
Formaat: Artigo
Taal:Inglês
Gepubliceerd in: Elsevier 2019
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Original article
Online toegang:https://ncbi.nlm.nih.gov/pmc/articles/PMC6663923/
https://ncbi.nlm.nih.gov/pubmed/31384539
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.apsb.2019.01.001
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