Bioorganic and Medicinal Chemistry Letters p. 844 - 847 (2019)
Update date:2022-08-03
Topics:
Wang, Xiaowen
Su, Mingbo
Li, You
Liu, Tongchao
Wang, Yujie
Chen, Yabing
Tang, Le
He, Yu-Peng
Ding, Xiaoguang
Yu, Fang
Shen, Jingkang
Li, Jia
Zhou, Yubo
Chen, Yue-Lei
Xiong, Bing
Tranylcypromine moiety extracted from LSD1 inhibitors and 6-trifluoroethyl thienopyrimidine moiety from menin-MLL1 PPI inhibitors were merged to give new chemotypes for medicinal chemistry study. Among 15 new compounds prepared in this work, some exhibited nanomolar LSD1 activity and good selectivity over MAO-A/B, low micromolar menin-MLL1 PPI inhibitory activity, as well as submicromolar MV4-11 antiprofilative activities. Intracellular LSD1 engagement of compounds with higher enzymatic and antiproliferative activities was confirmed by CD86 mRNA up-regulation experiments.
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