Design, synthesis and biological evaluation of [1,2,4]triazolo[1,5-a]pyrimidines as potent lysine specific demethylase 1 (LSD1/KDM1A) inhibitors
文摘
A new series of [1,2,4]triazolo[1,5-a]pyrimidine-based analogs were designed and synthesized. Compound 5p inactivated LSD1 potently (IC50 = 154 nM). Docking studies were performed to rationalize the potency against LSD1. Compound 5p inhibited migration of MGC-803 and PC-9 cells. Compound 6l showed excellent growth inhibition toward MGC-803 and PC-9 cells.