Cytotoxic activity of 5,7-dimethoxy-2-phenyl-N-propylquinolin-4-amine (DMPPQA) was investigated in human colon cancer cells HCT-116 and umbilical vein endothelial cell line HUVEC. The IC50 of DMPPQA on HCT-116 and HUVEC cells were respectively 1.26 and 7.43 µM after 72 h treatment. DMPPQA inhibited the growth of HCT-116 and HUVEC cells in concentration- and time-dependent manners. Typical morphological changes of apoptotic body formation were seen after DMPPQA with Hoechst 33258 staining. FCM analysis showed that DMPPQA induced apoptosis, mitochondrial membrane potential loss (ΔΨm) and increase in the production of intracellular reactive oxygen species (ROS) of HCT-116 cells. After treating with DMPPQA, apoptosis-related protein expression of Bax, cytochrome c, caspase-9, caspase-3, PARP-1 and P53 increased and Bcl-2 protein expression decreased. DMPPQA treatment of HUVECs reduced cell migration and microcapillary tube formation in a Matrigel matrix. It also decreased VEGF protein expression. Thus DMPPQA acts as an angiogenesis inhibitor and induces cell apoptosis by a caspase-dependent mitochondrial pathway.