This review reviews diagnostic applications and therapeutic on the use of based of dendrimer systems for anti-tumour therapy. Recent studies have shown that dendrimers are ideal delivery vehicles for explicit studies of the effects of polymer size, charge and composition and structure on biorelated properties like lipid bilayers interaction,plasma retention time, tumor absorption, biodistribution, cytotoxicity, and internalization. In the past few years, significant advances have been made in the treatment and diagnosis of dendrimers in the field of anticancer therapy. In this report, recently achievements in dendritic molecules in cancer therapy and diagnosis will be introduced, as well as the applications of dendritic molecules as a therapeutic platform for a variety of cancers, including chemotherapy, radiation therapy, photothermal therapy, photodynamic therapy, gene therapy and some other techniques.