Recent Updates on Novel Quinazoline‐Hybrid Molecules Possessing EGFR‐Mediated Anticancer Activity

ABSTRACT

As the first member of the receptor tyrosine kinase family, epidermal growth factor (EGFR) has been linked to human cancers through numerous lines of evidence. Research on EGFR has also led to the development of several key theories regarding cancer progression. Through a vast array of paracrine loops, each of which regulates a crucial stage in the metastasis cascade, EGFR not only maintains cell proliferation but also confers resistance to anti‐cancer cytotoxic treatments. To identify EGFR tyrosine kinase inhibitors (TKIs), simulation studies have been used to produce several small molecules, especially those containing quinazolines. The design process also evaluated the emergence of resistance problems and epigenetic changes, which eventually reduced drug efficacy and made it clear that more study in this field was required. The genetic changes taking place in the EGFR tyrosine kinase domain have been thoroughly studied in recent decades. These changes have made it possible to create highly effective inhibitors. The structure–activity relationship (SAR) and cytotoxic activity of several quinazoline derivatives with demonstrated EGFR‐inhibitory antiproliferative activity are highlighted in this review. In the present paper, we report the EGFR‐mediated anticancer potential of quinazoline derivatives discovered after 2020.