Original paper

4-Aminoindazolyl-dihydrofuro[3,4- d ]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase

Volume: 26, Issue: 2, Pages: 534 - 539
Published: Jan 1, 2016
Abstract
The treatment of epidermal growth factor receptor (EGFR)-driven non-small cell lung cancers with the T790M resistance mutation remains a significant unmet medical need. We report the identification of 4-aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of EGFR, with excellent activity against the T790M resistance double mutants and initial single activating mutants. Using an optimization strategy focused on structure-based...
Paper Details
Title
4-Aminoindazolyl-dihydrofuro[3,4- d ]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase
Published Date
Jan 1, 2016
Volume
26
Issue
2
Pages
534 - 539
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