Abstract

Introduction: The Epidermal growth factor receptor is a transmembrane glycoprotein that belongs to the ErbB family of tyrosine kinase receptors, which includes four EGFR members ErbB1 (HER₁/ErbB₁), ErbB₂ (HER₂/neu), ErbB3 (HER₃), and ErbB₄ (HER₄).

Methods: Amplification of EGFR corresponds to tyrosine kinase autophosphorylation that activates a downstream signalling pathway involved in regulating tumorigenesis, differentiation, and preservation.

Results: In cancer treatment, inhibition of EGFR is essential; therefore, potential EGFR inhibitors are required. Previously approved tyrosine kinase inhibitors such as erlotinib, lapatinib, and gefitinib and heterocyclic compounds such as pyrimidine, quinazolines, isoquinoline, purine, pyrazole, benzothiazole, imidazole, have received a lot of attention in cancer treatment due to their EGFR inhibition activity.

Conclusion: This review focuses on the diverse categories of synthetic entities compounds that were reported as potential EGFR and EGFR/ErbB-2 dual inhibitors. Furthermore, it will provide inexorable scope for investigators to design and synthesize potent EGFR inhibitors.

Keywords: EGFR, heterocycle, cancer, proliferation, apoptosis, EGFR inhibitors.