In order to increase the cell penetration and decrease the cytotoxicity of the synthetic molecule, we designed and synthesized a DNA-binding ligand, which was a conjugate of polyamide and phospholipid. We examined the differences in the effect on cytotoxicity between the conjugate and the native polyamide. As expected that the in vitro cytotoxicity of the conjugate was obviously lower than that of the native polyamide either in HeLa cells or SH-SY5Y neuroblastoma cells. In order to increase the cell penetration and decrease the cytotoxicity of the synthetic molecule, we designed and synthesized a DNA-binding ligand, which was a conjugate of polyamide and phospholipid. We examined the differences in the effect on cytotoxicity between the conjugate and the native polyamide. As expected that the in vitro cytotoxicity of the conjugate was obviously lower than that of the native polyamide either in HeLa cells or SH-SY5Y neuroblastoma cells.