Quinazoline is the main six-membered heterocyclic ring system reported for their biological activities, compounds with multiple pharmacophores, which bring together knowledge of a target with understanding of the molecule types that might interact with the target family. Robust, versatile and scalable chemistry must be employed to accomplish the task. This characteristic feature of quinazoline would make a good template for a lead generation library. The current review article focuses on biological actions done for various targets along with the brief description of the targets.