Discovery of vanadium complexes bearing tridentate schiff base ligands as novel LSD1 inhibitors |
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Authors: | Ling-Pan Lu Jin-Hai Liu Shi-Hong Cen Ya-Ling Jiang Guo-Qiang Hu |
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Institution: | School of Pharmaceutical Sciences, Zhengzhou University of Industrial Technology, Zhengzhou 451199, PR China |
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Abstract: | Lysine specific demethylase (LSD1) plays a pivotal role in epigenetic modulation of gene expression. Abberrant expression of LSD1 was associated with the progress and oncogenesis of multiple human cancers. Herein, we report the preliminary anti-LSD1 evaluation of the synthetic vanadium (V) complexes. Among them, complex 2 showed a moderate inhibitory effect against LSD1 with IC50 value of 19.0?μM, as well as good selectivity over MAO-A/B. Complex 2 is the first vanadium based LSD1 inhibitor, which provides a novel scaffold for the development of LSD1 inhibitor. |
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Keywords: | Vanadium complex LSD1 MAO Anticancer |
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