For the development of novel tetra-substituted aluminum phthalocyanine used as photodynamic therapy (PDT) photosensitizer with good photodynamic anticancer activity, tetraamino-, tetraacetamido-, tetrapropanamido- and tetrabutanamido-aluminum phthalocyanines are synthesized by phthalic anhydride-urea method with 4-nitro phthalic acid as preactant. The structures of these aluminum phthalocyanines are characterized. Their fluorescent spectra and acute toxicity are also measured. Meanwhile, their photodynamic anticancer activities are determined. As a result,the aluminum phthalocyanines are innoxious to mice. When 20 mg/kg aluminum phthalocyanines are injected to S180 sarcoma-bearing mice, the sensitizers show that the rates of inhibitory to S180 sarcoma are 44.96%, 45.87%, 45.62% and 48.65% respectively,which are in little difference according to the order of tetraamino-, tetraacetamido-, tetrapropanamido- and tetrabutanamido-phthalocyanine aluminum, respectively. While the concentration of injecton is raised to 40 mg/kg, the rates of inhibitory are 39.16%, 42.81%, 40.56% and 51.82% respectively for the same order. In this condition, tetrabutanamidophthalocyanine aluminum shows the highst PDT anticancer activitiy.