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. Thiophene, a sulfur containing heterocyclic scaffold, has emerged as one of the relatively well-explored scaffold for the development of library of molecules having potential anticancer profile. Thiophene analogs have been reported to bind with a wide range of cancer-specific protein targets, depending on the nature and position of substitutions. Accordingly, thiophene analogs have been reported to cause their biological action through inhibition of different signaling pathways involved in cancer. Functionally, different anticancer targets require different structural features, so researchers have tried to synthesize new thiophene derivatives with varied substitutions. In the present review, authors have presented the information available on thiophene-based molecules as anticancer agents with special focus on synthetic methodologies, biological profile and structure activity relationship (SAR) studies. Various patents granted for thiophene containing molecules as anticancer have also been included.
