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Letters in Drug Design & Discovery

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ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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Review Article

Emerging Heterocyclic Epidermal Growth Factor Receptor Inhibitors for the Management of Cancer: A Chemical Review

Author(s): Rupali Likhar*, Amey Deshpande, Tabassum Khan and Arati Prabhu

Volume 21, Issue 5, 2024

Published on: 08 May, 2023

Page: [866 - 879] Pages: 14

DOI: 10.2174/1570180820666230417093528

Price: $65

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.

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