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Issue 5, 2019
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Dual inhibitors of LSD1 and spermine oxidase

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We have previously described the synthesis and evaluation of 3,5-diamino-1,2,4-triazole analogues as inhibitors of the flavin-dependent histone demethylase LSD1. These compounds are potent inhibitors of LSD1 without activity against monoamine oxidases A and B, and promote the elevation of H3K4me2 levels in tumor cells in vitro. We now report that the cytotoxicity of these analogues in pancreatic tumor cells correlates with the overexpression of LSD1 in each tumor type. In addition, we show that a subset of these 3,5-diamino-1,2,4-triazole analogues inhibit a related flavin-dependent oxidase, the polyamine catabolic enzyme spermine oxidase (SMOX) in vitro.

Graphical abstract: Dual inhibitors of LSD1 and spermine oxidase

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The article was received on 12 Dec 2018, accepted on 06 Feb 2019 and first published on 08 Feb 2019

Article type: Research Article
DOI: 10.1039/C8MD00610E
Med. Chem. Commun., 2019,10, 778-790

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    Dual inhibitors of LSD1 and spermine oxidase

    S. Holshouser, M. Dunworth, T. Murray-Stewart, Y. K. Peterson, P. Burger, J. Kirkpatrick, H. Chen, R. A. Casero and P. M. Woster, Med. Chem. Commun., 2019, 10, 778
    DOI: 10.1039/C8MD00610E

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