Structure-based rational design and biological evaluation of a quinazoline-based EGFR exon 20 insertion inhibitor.
This study describes the structure-based design and synthesis of potent quinazoline-based inhibitors targeting EGFR exon 20 insertion (exon20ins) mutants, one of the challenging oncogenic drivers in non-small cell lung cancer (NSCLC). Guided by in silico modelling, a novel series of quinazoline analogues was designed t...