Thiazolidinedione (TZD) containing derivatives have been proved to be promising anticancer agents in preclinical and clinical evaluation phases. Hybrid molecules not just offer the benefits such as enhanced therapeutic effects and improved specificity, but in addition could beat drug resistance, so hybridization of thiazolidinedione scaffold with other anticancer pharmacophoric scaffolds may constitute a hopeful strategy to develop newer and more efficacious anticancer agents. Based on this approach, in past decade, several such hybrids containing TZD scaffold have been reported and evaluated for their antitumor activity, and some of them revealed excellent in vitro potency, indicating their potential as presumed anticancer drugs. This review summarizes the recent advances of TZD hybrids as potential anticancer agents, highlighting their antitumor activity and possible mechanism of action. Structure‐activity relationship (SAR) studies will also be discussed to direct the rational molecular hybridization of TZD scaffolds to design more effective candidates.