Autophagy is a self-renewal process in cells by recycling redundant materials through lysosomal machinery. The basal level of autophagy in eukaryotic cells plays a "housekeeping" role by degrading redundant cellular materials and providing nutrients and energy. However acute and sustained autophagy may cause autophagic cell death. These two features of autophagy are consistent with its complex roles in both oncogenesis and cancer development. Many small molecule autophagy regulators are developed to turn autophagy on/off for therapeutic purpose. The roles of chemotherapeutic agents in regulating autophagy and facilitating cancer treatment can be classified into three categories: direct autophagy enhancers, indirect autophagy enhancers and autophagy inhibitors. The representative autophagy regulators and their roles in cancer treatment were reviewed.