A series of quinazolin-2-amine derivatives (Ⅲa~Ⅲf) were synthesized by condensation, cyclization and so on from isolongifolanone and characterized by 1HNMR, 13C NMR, IR and HRMS. Their inhibitory activity against human hepatoma cell (HepG2) and human umbilical vein endothelial cells (HUVECs) were evaluated by MTT assay. The results showed that the half maximal inhibitory concentrations of compounds Ⅲa, Ⅲb, Ⅲd and Ⅲf were 8.58±0.5, 44.52±0.9, 57.18±0.8 and 32.83±0.6 μmol/L, indicating that these compounds showed moderate antitumor activity against HepG2. Among these compounds, compound Ⅲa, 4-(4'-chlorophenyl)-6,6,10,10-tetramethyl-5,6,6a,7,8,9,10,10a-octahydro-6a,9-methanobenzo[h]quinazolin-2-amine, had the best activity against HepG2. Only 4-(4'-(N,N-dimethylamino)phenyl)-6,6,10,10-tetramethyl-5,6,6a,7,8,9,10,10a-octahydro-6a,9-methanobenzo[h]quinazolin-2-amine (Ⅲf) showed a certain inhibitory activity against HUVECs. These compounds were also carried out to evaluate against myzus persicae by a leaf-dipping method. It was found that compounds Ⅲa and Ⅲd gave excellent insecticidal activity against myzus persicae with corresponding lethal concentration (LC50) of 37.4589±6.412 and 41.0073±5.920 mg/L.