Background: Cancer is spreading all over the world, and it is becoming the leading cause of major
deaths. Today’s most difficult task for every researcher is to invent a new drug that can treat cancer with minimal
side effects. Many factors, including pollution, modern lifestyle and food habits, exposure to oncogenic
agents or radiations, enhanced industrialization, etc. can cause cancer. Treatment of cancer is done by various
methods that include chemotherapy, radiotherapy, surgery and immunotherapy in combination or singly along
with kinase inhibitors. Most of the anti-cancer drugs use the concept of kinase inhibition.
Objective: The number of drugs being used in chemotherapy has heterocycles as their basic structure in spite of
various side effects. Medicinal chemists are focusing on nitrogen-containing heterocyclic compounds like pyrrole,
pyrrolidine, pyridine, imidazole, pyrimidines, pyrazole, indole, quinoline, oxadiazole, azole, benzimidazole,
etc. as the key building blocks to develop active biological compounds. The aim of this study is to attempt
to compile a dataset of nitrogen-containing heterocyclic anti-cancer drugs.
Methods: We adopted a structural search on notorious journal publication websites and electronic databases
such as Bentham Science, Science Direct, PubMed, Scopus, USFDA, etc. for the collection of peer-reviewed
research and review articles for the present review. The quality papers were retrieved, studied, categorized into
different sections, analyzed and used for article writing.
Conclusion: As per FDA databases, nitrogen-based heterocycles in the drug design are almost 60% of unique
small-molecule drugs. Some of the nitrogen-containing heterocyclic anti-cancer drugs are Axitinib, Bosutinib,
Cediranib, Dasatanib (Sprycel®), Erlotinib (Tarceva®), Gefitinib (Iressa®), Imatinib (Gleevec®), Lapatinib (Tykerb
®), Linifanib, Sorafenib (Nexavar®), Sunitinib (Sutent®), Tivozanib, etc. In the present review, we shall focus
on the overview of nitrogen-containing heterocyclic active compounds as anti-cancer agents.