Abstract: In 1920 Otto Warburg firstly described that even in the presence of ample oxygen, cancer cells prefer to metabolize glucose by glycolysis, which named as "Warburg effect". There are growing evidence supporting that the glycolysis pathway of cancer cells is closely associated with the tumorigenesis and development. The drugs targeting glycolytic enzymes and transporters can have an obviously anti-tumor effect by inducing tumor cells cycle arrest, apoptosis, regulating the autophagy of cancer cells and inhibiting the metastasis of the tumor. Many glycolytic enzymes and transporters can be suitable candidate targets for cancer therapy. The review is focused on the inhibitors of glycolysis reported in recent years, summerizes and outlooks the anti-tumor effect of these drugs.