Discovery of new tranylcypromine derivatives as highly potent LSD1 inhibitors.

Basic Information

ID: ALA4814040

Journal: Bioorg Med Chem Lett

Title: Discovery of new tranylcypromine derivatives as highly potent LSD1 inhibitors.

Authors: Huang MJ, Guo JW, Fu YD, You YZ, Xu WY, Song TY, Li R, Chen ZT, Huang LH, Liu HM.

Abstract: Tranylcypromine (TCP)-based structural modifications lead to the discovery of new LSD1 inhibitors, of which compounds 26b and 29b effectively inhibit LSD1 with the IC₅₀ values of 17 and 11 nM, respectively and also show good selectivity over MAO-B. Mechanistic studies showed that compound 29b concentration-dependently induced H3K4me1/2 accumulation in LSD1 overexpressed MGC-803 cells and also inhibited metastasis of MGC-803 cells. Collectively, both compounds could be promising lead compounds for further investigation.

CiteXplore: 33775841

DOI: 10.1016/j.bmcl.2021.127993

Patent ID: ┄

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