Heterocyclic compounds hold a pivotal place in medicinal chemistry due to their wide range of biological activities and thus, are exhaustively explored in the field of drug design and development. Continuous efforts are being carried out for the development of medicinal agents, especially for dreadful diseases like cancer. 4,5,6,7-Tetrahydrobenzo[b]thiophene has emerged as one of the relatively well-explored scaffold for the development of library of molecules having potential anticancer profile. 4,5,6,7-Tetrahydrobenzo[b]thiophene-based derivatives have been reported to bind with a wide range of cancer-specific protein targets, depending on the nature and position of substitutions. The review has uncovered 4,5,6,7-tetrahydrobenzo[b]thiophene as an incredible platform in the field of medicinal chemistry, particularly its anticancer profile, to offer detailed information to the researchers/scientists to plan and create novel, target-based and advanced thiophene analogs. A broad biological profile is shown by this scaffold that will prompt potential pharmaceutical agents. Thus, this review will help researchers to develop lead compounds in a different biological domain with a nidus on cancer chemotherapy.