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

Zhonghua Li, Lina Ding, Zhongrui Li, Zhizheng Wang, Feng‐Zhi Suo, Dandan Shen, Taoqian Zhao, Xudong Sun, Junwei Wang, Ying Liu,

Acta Pharmaceutica Sinica B · 2019 · 79 citations · 44 references

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Abstract

induced expression of CD86 and CD11b in THP-1 cells, confirming its cellular activity and ability of inducing differentiation. The findings further indicate that targeting LSD1 is a promising strategy for AML treatment, the triazole-fused pyrimidine derivatives are new scaffolds for the development of LSD1/KDM1A inhibitors.

References

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