| Literature DB >> 30713023 |
Xiaowen Wang1, Mingbo Su2, You Li3, Tongchao Liu4, Yujie Wang2, Yabing Chen5, Le Tang5, Yu-Peng He6, Xiaoguang Ding6, Fang Yu7, Jingkang Shen8, Jia Li2, Yubo Zhou9, Yue-Lei Chen10, Bing Xiong11.
Abstract
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.Entities:
Keywords: LSD1 inhibitor; MV4-11 antiproliferative activity; Menin-MLL1 protein-protein interaction inhibitor; Structure activity relationship; Tranylcypromine
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Year: 2019 PMID： 30713023 DOI： 10.1016/j.bmcl.2019.01.017
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823