Abstract: The pentose phosphate pathway (PPP) is an important pathway for the catabolism of glucose, serving as a bridge between glucose metabolism and nucleotide metabolism. PPP guarantees the supply of ribose for cell proliferation. Reports show that the key enzymes of PPP are generally highly expressed in tumor cells. Targeting PPP pathway has become an effective strategy for anti-tumor drug development. This paper reviews the current research progress of small-molecule inhibitors targeting key enzymes in the oxidative PPP, aiming to provide new ideas for drug development in related fields.