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.