Prospects of novel fourth-generation EGFR-TKIs overcoming C797S-mediated resistance in non-small cell lung cancer.
Insights into fourth generation selective inhibitors of (C797S) EGFR mutation combating non-small cell lung cancer resistance.
36 dibenzodiazepinone analogues were designed and synthesized, and their antiproliferative activities were evaluated. Compound 33 exhibited best inhibitory activity against Osimertinib resistant NSCLC cells.
The study summarizes the findings from the last eight years of research on heterocyclic core-based epidermal growth factor receptor inhibitors. This provides an invaluable tool for oncology drug discovery.
Small molecules targeting activating mutations within the epidermal growth factor receptor (EGFR) are efficacious anticancer agents, particularly in non-small cell lung cancer (NSCLC).