Muscimol, cycloserin and ibotenic acid which are extracted from mushroom contain isoxazole pharmacophore structure. By using muscarinic structure as a model compound and molecular recombination method, we synthesized muscarinic analogues compounds 3-(1',2'-di-O-isopropylidenedioxyethyl)-5-aryl-3a, 6a-dihydro-4,6-dioxopyrrolino[3',4'-d]isoxazoline derivatives through 1,3-dipolar cycloaddition reaction. The structures of the target compounds were confirmed by UV-Vis, ¹H NMR, IR and elemental analysis. The drug activities of obtained compounds were screened in vitro. The pharmacophore in the structure is a potential non-covalent DNA binding, the compounds have anticancer activity and the leukocyte common antigen activity in a different extent. The preliminary results of in vitro anticancer test suggest that the inhibitory rates of compounds 3a-3o to Cdc25A phosphatase in cell division cycle ranged from 56.99%-99.94%; at the test concentration of 20 μg·mL^-1, 3f, 3h, 3i, 3m, 3o were no inhibition activity, and the rest of the compounds shows moderate to good excellent inhibition rate from 66.85% to 99.84%, even at the concentration as low as 5 μg·mL^-1. At the test concentration of 20 μg·mL^-1, except compound 3i, the rest compounds' inhibition activity of against leukocyte common antigen (LCA) CD45 protein tyrosine phosphatase A, are 63.08%-92.09%. These active compounds are potential inhibitors against Cdc25A and CD45 protein tyrosine phosphatase A, which have great application prospects in the treatment of cancers and Inflammatory and immune diseases.