Cancer is the second leading cause of the death worldwide. As per the reports published by WHO, the cases of cancer in the world will increase to 22 million by 2030. Many resources are investigated all around the world for developing preventive, diagnostic and therapeutic strategies for cancer. Malignant cells display metabolic changes because of genetic and epigenetic alterations as compared to normal cell. Heterocycles are the key structural feature of many anti-cancer drugs present in the market. Between 2010 to 2015, FDA approved anticancer drugs also contain heterocyclic rings in their structures. Their presence in anti-cancer drugs can be credited to their being extremely common in nature, with enormous cellular processes and mechanisms. This review throws light on several heterocyclic compounds containing nitrogen, sulphur and oxygen in their rings, possessing anticancer activity on different cell lines. A compiled data of heterocyclic rings will help in providing a new way towards future development of new compound for treatment of cancer.