Pharmacophore conjugation strategy for multi-targeting metal-based anticancer complexes

Abstract Metal-based anticancer drugs play a very important role in clinical therapy. Classical platinum anticancer drugs bind to DNA, causing various kind of DNA damage so as to induce the cancer apoptosis. However, severe side effects and inherited or acquired resistance limit their application. As cancers are multiple factor induced diseases, drugs that act at multiple targets may exert higher efficacy and lower resistance. In recent years, multi-targeting anticancer drugs attract broad attention in drug development. Pharmacophore conjugation strategy is one of the most important way to design and obtain multi-targeting drugs. Its application in developing novel metal-based multi-targeting anticancer agents will be discussed in detail.