Recent achievements in molecular insights, anticancer activities, and comparative structure activity relationships of...

The EGFR family is considered one of the most important receptor tyrosine kinases. The family consists of four main members: EGFR, HER₂, ErbB₃, and ErbB₄. They have a crucial role in cancer progression and growth, especially in solid tumors such as lung, breast, colon, neck, and brain tumors. Since the first member, EGFR, is highly incorporated in several pathways regarding cancer, we provide a comparative understanding of all FDA-approved drugs targeting EGFR, demonstrating their structures' developments to provide a good illustration of possible EGFR binding interactions. From the recently approved drugs, we selected our nucleus for study, which is the thiazolidin-4-one nucleus. The review aims to provide an overview of all recent EGFR TK inhibitors bearing this nucleus with additional demonstrations of their structure-activity relationships gathering all those SARs into a general one. A comprehensive understanding of SARs of recent thiazolidin-4-one derivatives may inspire others to develop new, potent, and selective drugs targeting EGFR.