| abstract |
The invention belongs to the field of medicinal chemistry, and discloses barbituric acid compounds, a preparation method and an application thereof. Specifically, it relates to the compound represented by formula I and its medical use as a selective LSD1 reversible inhibitor, especially the application in the preparation of antitumor drugs. Tests have shown that the compound of formula I of the present invention can potently and reversibly inhibit the activity of LSD1, and has a weak inhibitory effect on the homologous proteins MAO-A and MAO-B, and can strongly induce the differentiation of leukemia cells NB4 and significantly enhance the LSD1 substrate Methylation levels of H3K4me1 and H3K4me2. |