Nitrogen‐Containing Heterocyclic Scaffolds as EGFR Inhibitors: Design Approaches, Molecular Docking, and Structure‐Activity Relationships

AbstractCancer is a wide collection of diseases and among the numerous pathways involved in cancer pathogenesis, pathway involving epidermal growth factor receptor (EGFR) is one of the most prominent. EGFR frequently articulated in a variety of cancer such as breast cancer, pancreatic cancer, non‐small cell lung cancer (NSCLC), head and neck cancer. There are different EGFR tyrosine kinase inhibitors (TKIs) approved by FDA for the treatment of cancer. However, none of them evidenced as boon to oncological and medical department. Frequently occurrence of inherent and acquired resistance of TKIs as a result of mutations is the principal cause for the current situation. Therefore, researchers are in the desire of evolving the novel EGFR TKIs. Further, N‐heterocyclic ring system always proved to be the magical weapon in designed and discovery of synthetic molecules as they acquired comprehensive range of pharmacological properties. In recent year (2018–2022) N‐heterocyclic derivatives were uncovered as the potential EGFR TKIs. The present review summarised the research progress of EGFR TKIs to dazed the limitations of currently accessible drugs by consecrating, anatomy, mutation of EGFR, and its role in different types of cancer. The review highlights the medicinal chemistry prospective emphasising about the designing strategies, docking studies, biological evaluation, selectivity and structural activity relationship of N‐heterocyclic compounds. Our review will support the medicinal chemists in direction for the development of novel N‐heterocyclic based EGFR TKIs.