Currently, the arise of drug resistance and undesirable offtarget effects of anti-cancer agents are major challenges for cancer treatment, which energizes medicinal chemists to develop more anticancer agents with high efficiency and low toxicity continuously. sulphonamide derivatives are a class of promising compounds with diverse biological activities including anti-cancer, and parts of them have been marketed for cancer therapy. In this review, we summed up the synthesis of sulphonamide derivates and their anticancer activities. Today Cancer remains to be one of the deadliest diseases in the world. Due to the potential anticancer activity of the campholinicaldehyde and sulfonamide moieties, five novel hybrid compounds containing both structures have been designed and synthesized in 3 steps. The synthesized compounds were characterized on the basis of IR, 1 H NMR, 13 C NMR spectral data, and elemental analysis and also, they were screened for invitro anticancer activity on human breast cancer cell line MCF-7 and HELA by the MTT assay method. Among them,4-fluoro-N-(4-(4-oxo-2-((2,2,3-trimethylcyclopent-3-en-1-yl) methyl) thiazolidine-yl)phenyl) benzene sulfonamide (Fig. 5b) showed the most potent anticancer activity against MCF-7 cell line. We hope this review could provide a clear insight for medicinal chemists in the rational design of more potent and bio-target specific anti-cancer agent.