Abstract: AimTo design and synthesize new arylsubstituted imidazolin-2-one analogues as antitumor compounds. MethodsArylsubstituted imidazolin-2-ones were prepared by condensation the appropriate ω-amino-acetophenone hydrochloride with arylisocyanate in toluene. The target compounds prepared in this study were tested for cytotoxicity against PC-3, A549, HO-8910, Hela, HL60, K562 and HL60R cancer cell lines, and mechanism of one of the products 4y was further evaluated with its mechanium. ResultsThirty-six new compounds were synthesized and confirmed by ¹H NMR, MS and elemental analysis. One of the synthesized products, compound 4y, displayed an encouraging selective activity against HL60 cells, and it was partlydue to the cell cycle arrest and cell apoptosis. Conclusion Compound 4y is worthy to be intensively studied.