Epidermal growth factor receptor inhibitors as potential anticancer agents: An update of recent progress

Area of Science:

• Oncology
• Medicinal Chemistry
• Molecular Biology

Background:

• Epidermal growth factor receptor (EGFR) is crucial in cell signaling pathways, regulating proliferation, angiogenesis, apoptosis, and metastasis.
• Existing EGFR inhibitors lack specificity, leading to adverse effects and necessitating new therapeutic strategies.
• Drug resistance, mutations, and selectivity challenges drive the search for novel EGFR inhibitor chemotypes.

Purpose of the Study:

• To review recent (2016-2021) progress in the discovery and development of diverse EGFR inhibitors.
• To summarize preclinical and clinical data, structure-activity relationships (SAR), and mechanistic studies.
• To propose strategies for designing novel, selective, and effective EGFR inhibitors.

Main Methods:

• Literature review of recent advancements in EGFR inhibitor research (2016-2021).
• Compilation of data on diverse structural classes of EGFR inhibitors, including pyrazoline, pyrazole, imidazole, pyrimidine, coumarin, and benzothiazole.
• Analysis of preclinical and clinical data, SAR, mechanistic insights, and in silico studies.

Main Results:

• Identification of various structural classes of novel EGFR inhibitors with therapeutic potential.
• Summary of structure-activity relationships (SAR) for different inhibitor classes.
• Inclusion of mechanistic and in silico studies to guide future drug design.

Conclusions:

• Recent progress offers significant scope for developing novel EGFR inhibitors with enhanced selectivity and efficacy.
• Targeting EGFR remains a key strategy in cancer therapies for lung, breast, and other cancers.
• Further research into novel chemotypes and SAR is essential for advancing EGFR inhibitor development.