An Updated Mini-Review: Newer Quinazoline Based EGFR Inhibitors as Anticancer Agents

Introduction: Cancer remains one of the most prevalent and deadly illnesses, even with notable advancements in novel treatment alternatives. One important strategy for targeted cancer therapy is the EGFR (epidermal growth factor receptor) signaling pathway. Cancer treatment has greatly improved when the EGFR-driven pathway is inhibited by targeting the tyrosine kinase domain of EGFR. Several small compounds, particularly quinazoline-containing derivatives, have been developed using simulation studies to determine EGFR tyrosine kinase inhibitors (TKIs). The design process also assessed the appearance of epigenetic alterations and resistance issues, which limited the effectiveness of medications over time and clarified the necessity for additional research in this area. In recent decades, extensive research has investigated the genetic alterations occurring in the EGFR tyrosine kinase domain. These alterations have paved the way for the development and production of highly potent and efficacious inhibitors. Methods: This review highlights the structure-activity relationship (SAR) and biological activity of different quinazoline derivatives that have been reported to have EGFR-TK inhibitory antiproliferative activity. We searched Embase, Cochrane, and PubMed for literature on quinazoline derivatives showing EGFR inhibition as anticancer agents. Results: We confirmed that quinazoline derivatives with different substitutions are useful pharmacophores as EGFR TK inhibitors for achieving strong anticancer activity after a thorough review of the literature. Discussion: This review offers insights into the latest advancements in developing novel and potent quinazoline derivatives as potential EGFR tyrosine kinase inhibitors, which could be further optimized to develop new EGFR inhibitors in the future. Conclusion: Quinazoline-based scaffolds remain promising leads for developing nextgeneration EGFR tyrosine kinase inhibitors with enhanced anticancer efficacy.