Article
Synthesis and evaluation of osimertinib derivatives as potent EGFR inhibitors.
Bioorganic & medicinal chemistry - 1 Sept 2017
Gao Hongying, Yang Zimo, Yang Xinglin, Rao Yu
Abstract excerpt
Osimertinib has been identified as a promising therapeutic drug targeting for EGFR T790M mutant non-small cell lung cancer (NSCLC). A new series of N-oxidized and fluorinated osimertinib derivatives were designed and synthesized. The cellular anti-proliferative activity, kinase inhibitory activity and the activation of EGFR signaling pathways of 1-6 in vitro were determined against L858R/T790M and wild-type EGFR,...
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