The Benzopyrones are a group of compounds whose members include Coumarins and flavonoides. Dietary exposure to benzopyrones is quite significant, as these compounds are found in vegetables, fruit, seeds, nuts, coffee, tea and wine. It is estimated that the average western diet contains approximately 1g/day of mixed benzopyrones. It is, therefore, not difficult to see why extensive research into their pharmacological and therapeutic properties is underway over many years. Coumarin is a natural substance that has shown anti-tumour activity in vivo, with the effect believed to be due to its metabolites (e.g. 7-hydroxycoumarin). This review is based on recent studies of Coumarins and Coumarin related compounds. Therefore, the focus will be on these relevant compounds and their therapeutic importance along with the various methods of synthesis.