Abstract: As a critical DNA-repair enzyme, poly(ADP-ribose) polymerase(PARP) has been validated as an important target for the development of anti-cancer drugs. PARP inhibitors could effectively kill cancer cells through inhibiting DNA repair and synergistic lethal effect, and have been widely used for the treatment of various cancers. However, most of the approved PARP inhibitors displayed severe side effects due to their poor selectivity for PARP-1 over PARP-2. Therefore, decreased side effects could be achieved by improving the selectivity for PARP-1. In this article, discussion on recent research progress including research methods, structure-activity relationships and pharmacological effects of reported selective PARP-1 inhibitors will be reviewed.