Current Issues in Pharmacy and Medical Sciences · Published 2025-05-21 · DOI 10.12923/cipms-2025-0018
The Epidermal Growth Factor Receptor (EGFR) is responsible for cell differentiation and proliferation upon activation when it binds to one of its ligands. It is thought to be involved tumorigenesis, which is implicated in cancers such as lung cancer and breast cancer. Over the past decades, the EGFR has become extensively examined as a target for the development of new anticancer agents. Several EGFR tyrosine kinase inhibitors (TKIs) have been identified and assessed in clinical trials as potential treatments for carcinoma. This review provides updated information on Novel heterocyclic scaffolds, which are now considered important pharmacophores that have demonstrated significant potency as EGFR inhibitors. Kinase inhibitors, in the last few years, have emerged as emerging anticancer agents with promising results. In this review, we briefly discussed heterocyclic scaffolds and the structural activity relationships of lead compounds such as substituted quinazoline, pyrimidine, quinoline and indole as EGFR kinase inhibitors, as well as their use as anticancer agents. Information on miscellaneous heterocyclics such as thiazolyl-pyrazoline derivatives, pyrazole derivatives and oxadiazole derivatives is also included.
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