Microwave-assisted synthesis of numerous bioactive scaffolds has gained much attention of late in organic chemistry. Most of the heterocyclic rings can be synthesized using the microwave irradiation method. This application is further used in the synthesis of active pharmaceutical ingredients containing heterocycle moiety. These bioactive heterocyclic derivatives synthesized by microwave-assisted one-pot multicomponent reaction, have significant anticancer, antibacterial, and antimicrobial properties. Herein, we summarize significant advances in the microwave-assisted synthesis of heterocycles and their useful bioactive properties. Microwave-assisted bioactive heterocycles synthesis provides multi-component synthetic access to a large number of organic molecules having anti-cancer, anti-fungal, anti-bacterial, and other bio-activities. The microwave irradiation, ligand, catalyst, substrate, and reaction conditions were used to regulate the formation of numerous aza, oxa, and mixed heterocycles with different ring sizes and acyclic system with good yields, demonstrating the elegance, impact, and practicality of this microwave protocol. Display omitted