Abstract: Thirty-three compounds were designed and synthesized directly from three-component, one-pot condensation of 1-(4-methylphenyl)ethanone and aromatic amines with some aromatic aldehydes. The chemical structures of the Mannich bases were confirmed by ¹H NMR, IR and MS. The screening results of bioactivity indicated that all of these title compounds possessed the inhibitory activity at the concentration of 1×10^-4 mol·L^-1. Among them, the compound TM33 displayed the strongest bioactivity with the inhibition percentage of 60.3% against P338 cancer cell line at the concentration of 1×10^-8 mol·L^-1, and the value of the half maximal inhibitory concentration (IC₅₀) was as low as 0.45 nmol·L^-1. This study suggests a new type of potential anti-leukemia molecules.