BMX, a member of the Tec family of kinases, plays a pivotal role in the occurrence and progression of cancers and multiple chronic inflammations. However, there are rarely BMX inhibitors reported, and the signaling pathways mediated by BMX are still poorly understood. In this study, a series of novel BMX inhibitors bearing the core of 1,3,5-triazin-2-amine were designed and synthesized by structural modifications from the lead compound