Abstract: OBJECTIVE To synthesis and evaluate a series of novel phosphoramide compounds, and to evaluate their in vitro inhibitory activity of leukemia in K562 cells. METHODS The target compounds were designed by using aryl amino as active group while hydroxyproline as carrier moiety, they were synthesized by several nucleophilic substitution reaction, whose structures were characterized, the inhibitory effects of which on human chronic myeloid leukemia cell line K562 were determined by MTT assay. RESULTS Ten new compounds exhibited certain biological activity against K562 cells. CONCLUSION A new class of phosphoramide leading compounds with certain anti-tumor activity is found.