The review covers different synthetic approaches for thiazolidinone-4-one derivatives with their anticancer activity was also discussed in this paper. Thus, this study may assist to produce more potent and efficient thiazolidinone-4-one derivatives compounds as anticancer agents. Accessible information can be utilized as a practical clue for the rational design of novel small molecules with potent biological activity among thiazolidin-4-ones nucleus. The Research & Development in the area of anticancer is occurring towards the path where the new elements are created which are low in toxicity and are with further developed action. Thiazolidinone-4-one and its derivatives signify a very imperative class of heterocyclic compounds, which have miscellaneous therapeutic actions. As of late, numerous dynamic mixtures incorporated are extremely compelling; with thiazolidinone-4-one moiety have likewise demonstrated to be powerful towards malignant growth