Abstract: Prodrug modification is an effective strategy to improve chemotherapeutic drugs by increasing their tumor targetability, reducing side effects, and enhancing anticancer activity. The demand of tumor cells for glucose is much higher than that of normal cells, which is known as Warburg effect. Glucose transporters or receptors are over-expressed in many cancer cells, and the levels of some glycosidases are elevated in certain tumor tissues. As a result, glycoconjugate prodrugs are able to achieve targeted delivery of anticancer drugs. In recent years, with the accelerating development of multitarget and multifunctional glycoconjugate prodrugs, well-designed prodrugs with excellent tumor targetability are emerging, and the treatment scope of glycoconjugate prodrugs is broadening to many non-cancer diseases. In this paper, the research progress and prospect in small molecule glycoconjugate prodrugs is reviewed.