Identification of PR-SET7 and EZH2 selective inhibitors inducing cell death in human leukemia U937 cells

► Chemical manipulations made on broad HMT inhibitors afforded compounds more selectively. ► Bis(dibromo) analogs 5 and 10 showed selective activity against PR-SET7. ► Bis(monobromo) analogs 4 and 9 showed dual PR-SET7 and EZH2 inhibition. ► Bis(monobromo) analog 4 induced massive cell death in U937 cells.