Synthesis and antitumor activity of phosphonate derivatives containing amino acid

In search of effective anticancer agents, fifteen new phosphonate derivatives were designed and synthesized. Their structures were clearly established by elemental analysis, IR, ¹H NMR and ¹³C NMR, and their antitumor activities were evaluated by MTT assay. Preliminary results in bioactivity tests indicated that some title compounds exhibited better activity. Among the active compounds, compounds 4e, 4n had better inhibition effect on A-549 cells growth with IC₅₀ values of 8.7±0.8, 8.2±1.0 μmol·L^-1, the IC₅₀ values of compound 4c was 9.8±0.9 μmol·L^-1 against SGC-7901 cells and compounds 4l, 4n exhibited more potent activities against EC-109 with IC₅₀ values of 9.5±0.6, 9.4±0.5 μmol·L^-1.