Increased glycolysis in malignant tumors has been one of the hallmarks and biotargets of tumor targeting that enable the design and development of novel targeted therapy agents. In this review, by focusing on the Warburg effect-targeted drug discovery and the unique concepts for development of glucose transporters(GLUTs)-targeted anticancer agents, we examine the current scenario with a brief introduction of anticancer GLUTs inhibitors and glycoconjugated antitumor examples, to provide an overview of studies of the Warburg effect-targeted anticancer drug development, the design strategy and useful perspectives for new-generation of targeted chemotherapeutic agents.