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• W2038434818 abstract "The clinical success of covalent kinase inhibitors in the treatment of EGFR-dependent non-small cell lung cancer (NSCLC) has rejuvenated the appreciation of reactive small molecules. Acquired drug resistance against first-line EGFR inhibitors remains the major bottleneck in NSCLC and is currently addressed by the application of fine-tuned covalent drugs. Here we report the design, synthesis and biochemical evaluation of a novel class of EGFR inhibitors with a covalent yet reversible warhead. A series of WZ4002 analogs, derived from anilinopyrimidine and 3-substituted-2-cyanoacrylamide scaffolds, exhibit strong and selective inhibitory activity against clinically relevant EGFR(L858R) and EGFR(L858R/T790M)." @default.
• W2038434818 created "2016-06-24" @default.
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• W2038434818 date "2015-06-01" @default.
• W2038434818 modified "2023-09-24" @default.
• W2038434818 title "Structure-based design and synthesis of covalent-reversible inhibitors to overcome drug resistance in EGFR" @default.
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• W2038434818 doi "https://doi.org/10.1016/j.bmc.2015.04.038" @default.
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