Despite extensive investigations in the field of cancer diagnosis and therapy in recent decades, cancer is still the major cause of morbidity and mortality all over the world. Recently, with the advancement of nanotechnology, the design and preparation of efficient nano-sized structures with the potential for diagnosis and treatment of cancer have been proposed. Among the different types of nano-sized materials, biocompatible polymers seem to be innovative tools with huge potential for cancer treatment. Advances in polymer chemistry and the application of various organic reactions have enabled the design and tailoring of multifunctional polymeric platforms with controllable architectures, with the ability to carry anticancer drugs, labelling probes and targeting agents simultaneously. This review covers the latest advances in the conjugation of the most studied chemotherapeutics (such as doxorubicin, paclitaxel, methotrexate, fluorouracil and cisplatin) to common dendritic polymers, including polyamidoamine dendrimers and hyperbranched polyglycerols (PGs) and their linear analogues, producing fatal weapons against tumors, with a focus on their cytotoxicity, biodistribution and biodegradability.