Title:An Updated Mini-review: Newer Quinazoline Based EGFR Inhibitors as Anticancer Agents
Volume: 23
Author(s): Sonali S. Shinde*, Sachin S. Bhusari and Pravin S. Wakte
Affiliation:
- Department of Chemical Technology, Dr. Babasaheb Ambedkar Marathwada University, Chhatrapati Sambhajinagar, 431004 (MS), India
Keywords:
EGFR inhibitors, tyrosine kinase, quinazoline pharmacophore, anticancer agents, quinazoline derivatives, antiproliferative activity.
Abstract:
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.
