Structure-Based Design of 5-Methylpyrimidopyridone Derivatives as New Wild-Type Sparing Inhibitors of the Epidermal Growth Factor Receptor Triple Mutant (EGFRL858R/T790M/C797S)

Abstract excerpt

Tertiary EGFR C797S mutation induced resistance against osimertinib ( 1 ) is an emerging “unmet clinical need” for non-small-cell lung cancer (NSCLC) patients. A series of 5-methylpyrimidopyridone derivatives were designed and synthesized as new selective EGFR L858R/T790M/C797S inhibitors. A representative compound, 8r-B, exhibited an IC 50 of 27.5 nM against the EGFR L858R/T790M/C797S mutant, while being a...

Topics

Share this publication in a Topic to start or enrich a Post.

• Share to Cancer therapeutics and mechanisms
• Share to Colorectal Cancer Treatments and Studies
• Share to Lung Cancer Treatments and Mutations