Structural modifications on indole and pyrimidine rings of osimertinib lead to high selectivity towards L858R/T790M double mutant enzyme and potent antitumor activity
Qiao Liu, Yanli Luo, Zerui Li, Chen Chen, Lei Fang
Topics & Concepts
OsimertinibChemistryT790MLead compoundPyrimidineMutantIn vivoIC50PharmacologyBiochemistryIn vitroEpidermal growth factor receptorReceptorErlotinibGefitinibBiologyBiotechnologyGeneLung Cancer Treatments and MutationsCancer therapeutics and mechanismsPI3K/AKT/mTOR signaling in cancer