氟化反苯环丙胺类似物作为赖氨酸特异性去甲基化酶1（LSD1，KDM1A）的抑制剂
Fluorinated tranylcypromine analogues as inhibitors of lysine-specific demethylase 1 (LSD1, KDM1A).
作者信息
Borrello Maria Teresa, Schinor Benjamin, Bartels Katharina, Benelkebir Hanae, Pereira Sara, Al-Jamal Wafa T, Douglas Leon, Duriez Patrick J, Packham Graham, Haufe Günter, Ganesan A
机构信息
School of Pharmacy, University of East Anglia, Norwich Research Park, Norwich NR4 7TJ, United Kingdom.
Organisch-Chemisches Institut, Universität Münster, Corrensstraβe 40, Germany; Cells-in-Motion, Cluster of Excellence, University of Münster, Waldeyerstraβe 15, 48149 Münster, Germany.
出版信息
Bioorg Med Chem Lett. 2017 May 15;27(10):2099-2101. doi: 10.1016/j.bmcl.2017.03.081. Epub 2017 Mar 29.
We report a series of tranylcypromine analogues containing a fluorine in the cyclopropyl ring. A number of compounds with additional m- or p-substitution of the aryl ring were micromolar inhibitors of the LSD1 enzyme. In cellular assays, the compounds inhibited the proliferation of acute myeloid leukemia cell lines. Increased levels of the biomarkers H3K4me2 and CD86 were consistent with LSD1 target engagement.
我们报道了一系列在环丙基环中含有氟的反苯环丙胺类似物。许多在芳环上具有额外间位或对位取代的化合物是LSD1酶的微摩尔级抑制剂。在细胞试验中，这些化合物抑制了急性髓系白血病细胞系的增殖。生物标志物H3K4me2和CD86水平的升高与LSD1靶点的作用一致。
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