Schiff bases and their transition metal complexes play an important role in the field of medicine, in particular in the treatment of cancer. Since the discovery of the cisplatin anticancer activity, great efforts have focused on the rational design of metal-based anticancer drugs that can be potentially used for the treatment of cancer. However, drug resistance and significant side effects greatly limit its clinical application. This has inspired medicinal chemists to employ various strategies in the development of novel and effective anticancer drugs. Recently, a greater number of transition metal complexes have been designed and evaluated for their anticancer activities, and some of them were at different stages of clinical studies. Amongst these, platinum, palladium, gold and silver complexes have an important place within medicinal and inorganic chemistry. This review article discusses Schiff bases and their complexes with selected transition metals (Pd, Pt, Ag, Au) for anticancer activity against different cancer cell lines.