Abstract: Energy metabolism of cancer cells is different from that of normal ones and aerobic glycolysis rather than oxidative phosphorylation is preferred in cancer cells as the pathway of glucose metabolism. This unique pathway may thus provide potential targets for anticancer drugs. Metal complexes represented by platinum-based anticancer drugs play an important role in the treatment of cancers due to their distinct structural diversity and antitumor activity. Since the existing metallodrugs with DNA as the target tend to induce drug resistance and systemic toxicity, it is necessary to design and discover novel metal antitumor drugs with alternative targets. The emergence of metal complexes targeting the energy metabolism of tumor cells in recent years represents the pertinent attempt made to meet the demand.