Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors

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Strategies to overcome acquired resistances conferred by mutations in the kinase domain of EGFR.Utilization of Structure-Based Design to Identify Novel, Irreversible Inhibitors of EGFR Harboring the T790M Mutation.

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P2860

Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors

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2015年論文

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2015年論文

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Oxopyrido[2,3-d]pyrimidines as ...... tor Receptor (EGFR) Inhibitors

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Oxopyrido[2,3-d]pyrimidines as ...... tor Receptor (EGFR) Inhibitors

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Oxopyrido[2,3-d]pyrimidines as ...... tor Receptor (EGFR) Inhibitors

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Oxopyrido[2,3-d]pyrimidines as ...... tor Receptor (EGFR) Inhibitors

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Oxopyrido[2,3-d]pyrimidines as ...... tor Receptor (EGFR) Inhibitors

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Oxopyrido[2,3-d]pyrimidines as ...... tor Receptor (EGFR) Inhibitors

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P2093

Andrew S Tasker

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Andrew T Parsons

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Brad Herberich

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Darren L Reid

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David Bauer

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David J St Jean

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Dean Hickman

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Dina A Andrews

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Edward K Lobenhofer

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Essa Hu-Harrington

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P2860

The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP

Part 1: Structure-Activity Relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase

Novel mutant-selective EGFR kinase inhibitors against EGFR T790M

Discovery and evaluation of 7-alkyl-1,5-bis-aryl-pyrazolopyridinones as highly potent, selective, and orally efficacious inhibitors of p38alpha mitogen-activated protein kinase

Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR)

Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC.

AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer

Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions

Epidermal growth factor receptor mutations in lung cancer

Covalent modifiers: an orthogonal approach to drug design.

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scholarly article

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10.1021/ACSMEDCHEMLETT.5B00193

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Simon J Hedley

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2015-07-27T00:00:00Z

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282278295

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26396685

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Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors

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P2860

P2860

Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors

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