36 dibenzodiazepinone analogues were designed and synthesized, and their antiproliferative activities were evaluated. Compound 33 exhibited best inhibitory activity against Osimertinib resistant NSCLC cells.
Prospects of novel fourth-generation EGFR-TKIs overcoming C797S-mediated resistance in non-small cell lung cancer.
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.
Insights into fourth generation selective inhibitors of (C797S) EGFR mutation combating non-small cell lung cancer resistance.
The development of EGFRC797S/L858R/T790M mutation has become a major barrier to tyrosine kinase inhibitors.