In search of more effective anticancer agents, according to the combination principle, 9 phosphonate derivatives were designed and synthesized. Their structures were clearly established by elemental analysis, IR, 1HNMR and 13CNMR, and their antiproliferative activities were evaluated against some tumor cell lines by using a methylthiazolyldiphenyl- tetrazolium bromide (MTT) method. Preliminary results in bioactivity tests indicated that they exhibited certain antitumor activities. Among the active compounds, compounds Ⅲf, Ⅲi had better inhibition effect on cells growth, espectively, compounds Ⅲi showed remarkable activities against A-549, SGC-7901 and EC-109 with IC50 values of 7.0±0.8, 6.9±0.8 and 7.3±0.7 μmol/L respectively, similar to cisplatin, which were worth further investigation.