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Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors.

Bioorganic & medicinal chemistry letters - 15 Nov 2021

Hoogenboom Niels, Demont Dennis, de Zwart Edwin, Verkaik Saskia, Emmelot Maaike, van de Kar Bas, Kaptein Allard, Barf Tjeerd

Abstract excerpt

Epidermal growth factor receptor (EGFR) inhibitors have clinical utility in the treatment of non-small cell lung cancer (NSCLC) patients. Despite encouraging clinical efficacy with these agents, many patients develop resistance due to sensitizing (or activating) mutations ultimately leading to disease progression. In the majority of the cases, this resistance is due to the T790M mutation and frequently coexisting...

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PMID: 34624491
DOI: 10.1016/j.bmcl.2021.128406

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