Based on the structure-activity relationships and antiangiogenic mechanism of RGD-containing peptides, a series of 5-amino-1,3-dihydro-1,3-dioxo-2H-isoindole derivatives were synthesized. The structures were characterized by 1H NMR, MS and elementary analysis. There ability to inhibit angiogenesis were evaluated by chick embryo chorioallantoic membrane assay at 10-5 mol/L. Compounds 7a and 7b displayed obvious antiangiogenic activity.