Cancer has been the most devastating disease for human beings for long time. Million people lost their lives due to cancer. Among the many anticancer drugs available today are heterocycles. Infact, the two third of the FDA approved new chemical entitites for cancer between 2010 and 2018 have heterocyclic rings in their structures. This have poised them as an important foundation of medicinal chemistry. Some market selling heterocyclic anticancer drugs include 5-flourouracil, methortrexate, Sofosbuvir, Aripiprazole, doxorubicin,Rosuvastatin daunorubicin, etc. Besides, some natural products such as vinblastine and vincristine are also used as anticancer drugs. Overall, heterocyclic moeities have always been core parts in the expansion of anticancer drugs. It has been found that there are a variety of heterocyclic compounds were used as anticancer agents. Heterocycles ring structures composed of elements other than carbon, where the most frequent substituents are oxygen, nitrogen and sulfur. Among the heterocyclic compounds the pyrimidines, pyrazoles, thiophene, pyridine, thiazole derivatives showed high cytotoxicity towards the cancer cell lines.General applications of heterocycles are very vast as they are diverse in nature. Apart from antitumor activity, heterocyclic compounds have a considerable active role as anti-bacterial, anti-viral, anti-fungal, anti-inflammatory etc.In this review, we provide for a concise overview of heterocyclic active compounds and families and their main applications in medicine.

Keywords: cancer therapy; heterocyclic compounds; oxygen, Sulphur and nitrogen-based heterocycles; NCE’s, Marketed Drugs.