Design, synthesis and biological evaluation of novel aminopyrimidine derivatives as potent EGFRC797S inhibitors for overcoming osimertinib resistance.
EGFRC797S mutation and bypass pathway activation are major drivers of acquired resistance to osimertinib; however, no approved therapeutic agents are currently available to effectively overcome this resistance. In this study, a series of aminopyrimidine-based small-molecule inhibitors were rationally designed and synth...