Several five and six-membered aromatic systems with three heteroatoms such as S, O, and N have been intensively researched due to their intriguing pharmacological properties. Heterocyclic compounds are chemicals that allow life to exist. Aside from that, all heteroatoms in the ring interact better with amino acids, and these interactions aid in reducing transactivation, and enhancing lipophilicity, solubility, and absorption, all of which can be exploited to improve therapeutic action. Heterocyclic nucleus 1,3,4-thiadiazole, benzimidazole, quinazoline, and pyrimidine derivatives have shown considerable biological actions such as anticancer, antimicrobial, anti-inflammatory, antidepressant, antioxidant, antifungal, antimicrobial, Carbonic anhydrase inhibitors, anticonvulsant, antibacterial activity, etc. All ring system members play a significant role in the development of novel drugs. In this review, we have highlighted the FDA approved drugs of heterocyclic compound which will pave the way for development of new entities. The current analysis focuses on synthetic derivatives of thiadiazole, benzimidazole, quinazoline, and pyrimidine that have significant anticancer biological effects on several cancer cell lines.