Quinazolinones as allosteric fourth-generation EGFR inhibitors for the treatment of NSCLC
Thomas W. Gero, David E. Heppner, Tyler S. Beyett, Ciric To, Seth C. Azevedo, Jaebong Jang, Thomas B. Bunnell, Frédéric Féru, Zhengnian Li, Bo Hee Shin, Kara M. Soroko, Prafulla C. Gokhale, Nathanael S. Gray, Pasi A. Jänne, Michael J. Eck, David A. Scott
Topics & Concepts
ChemistryAllosteric regulationQuinazolinoneT790MEGFR inhibitorsPotencyPharmacologyStructure–activity relationshipEpidermal growth factor receptorMutantMutagenesisMutationStereochemistryIn vitroBiochemistryGefitinibReceptorMedicineGeneQuinazolinone synthesis and applicationsLung Cancer Treatments and MutationsCancer therapeutics and mechanisms