Dihydroquinazolinones is an important core structure reported with a wide variety of pharmacological activities. They are capable of undergoing various transformations because of its reactivity towards various reagents. The synthetic strategies for the functionalization and derivatization of the nucleus were explained. The diversified pharmacological actions of this moiety were illustrated through various biochemical pathways. The structural-activity relationship study of dihydroquinazolinones anticipated the relationship between the various substituents and its role in the pharmacological action. The main objective of this review is to summarize the importance of dihydroquinazolinones in the field of chemical biology.