Cancer is the second leading cause of death in Iran, next to heart disease. Current therapy suffers from the major limitations of side effects and drug resistance, so the characterization of new structures that can be power-selective and less-toxic anticancer agents is the main challenge to medicinal chemistry research. Furoxan (1,2,5-oxadiazole-2-oxide) is a crucial compound with many medicinal and pharmaceutical properties. The most important aspect of furoxan is the nitric oxide (NO) molecule. One of the most essential furoxan derivatives, which could be utilized in medicinal goals and pharmaceutical affairs, is benzofuroxan. Furoxan could be described as a NO-donating compound in a variety of reactions, which could also appear as hybridised with different medicinal compounds. This review article presents a summary of syntheses and antitumor properties of furoxan derivatives as possible chemotherapy agents for cancer. Furoxan can inhibit tumor growth in vivo without any side effects in normal cells. Furthermore, due to NO-releasing in high levels in vivo and a wide range of anticancer compounds, furoxan derivatives and especially its hybridised compounds could be considered as antitumor, cytotoxic and apoptosis compounds to be applied in the human body.