The chemical class of benzopyrones consists of a large number of compounds possessing the benzene ring fused with the oxygen containing pyrone ring. This class is further divided into the benzo-γ-pyrone i.e. flavonoids and the benzo-α-pyrone i.e. coumarins. Coumarins, the 2H-chromen-2-one and its related analogues exhibit a multitude of biological activities. Attempts made in the continuous chemical diversification of this parent nucleus have brought significant alterations in the biological activity among the generated compounds and therefore, this category of benzopyrones has been much exploited in the current medicinal chemistry research. Thus, it was thought worthwhile to present a review on the newly synthesised heterocyclic coumarinyl derivatives with their physicochemical parameters and biological activity, attempted by our co-workers. This review also creates a platform for highlighting approaches and strategies used in the chemical synthesis of coumarinyl compounds along with their biological activity relating to their structure.