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Cancer is considered as the main challenge of human communities, and it annually imposes a significant economic burden on society. Natural products have been used for treatment of many diseases including inflammation, infections, neurological disorders, atherosclerosis, asthma and cancer for many years. Sesquiterpene lactones (STLs) refers to a group of natural products with different biological activities. A type of STL that has recently attracted much attention is Alantolactone (ALT). In recent years, many studies have investigated the molecular mechanism of this compound affecting cancer cells and results suggest that this compound exerts its anticancer effects by providing free radicals and inhibiting some of the signaling pathways that are effective in progression of cancer cells. The present study is aimed to introduce the latest molecular mechanisms of ALT proposed by researchers in recent years.