Design, Synthesis, and Evaluation of Ribose-Modified Anilinopyrimidine Derivatives as EGFR Tyrosine Kinase Inhibitors

Trisubstituted Imidazoles with a Rigidized Hinge Binding Motif Act As Single Digit nM Inhibitors of Clinically Relevant EGFR L858R/T790M and L858R/T790M/C797S Mutants: An Example of Target Hopping

(2017) Michael Juchum et al.   JOURNAL OF MEDICINAL CHEMISTRY

Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site

(2017) Marcel Günther et al.   JOURNAL OF MEDICINAL CHEMISTRY

Lung Cancer: EGFR Inhibitors with Low Nanomolar Activity against a Therapy-Resistant L858R/T790M/C797S Mutant

(2016) Marcel Günther et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Recent progress on third generation covalent EGFR inhibitors

(2016) Hengmiao Cheng et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors

(2016) Yong Jia et al.   NATURE

Acquired Resistance to the Mutant-Selective EGFR Inhibitor AZD9291 Is Associated with Increased Dependence on RAS Signaling in Preclinical Models

(2015) C. A. Eberlein et al.   CANCER RESEARCH

The Allelic Context of the C797S Mutation Acquired upon Treatment with Third-Generation EGFR Inhibitors Impacts Sensitivity to Subsequent Treatment Strategies

(2015) M. J. Niederst et al.   CLINICAL CANCER RESEARCH

Generations of Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors: Perils and Progress

(2015) Emily H. Castellanos et al.   CURRENT TREATMENT OPTIONS IN ONCOLOGY

Acquired EGFR C797S mutation mediates resistance to AZD9291 in non–small cell lung cancer harboring EGFR T790M

(2015) Kenneth S Thress et al.   NATURE MEDICINE

Heterogeneity Underlies the Emergence of EGFRT790 Wild-Type Clones Following Treatment of T790M-Positive Cancers with a Third-Generation EGFR Inhibitor

(2015) Z. Piotrowska et al.   Cancer Discovery

The next generation of epidermal growth factor receptor tyrosine kinase inhibitors in the treatment of lung cancer

(2014) Conor E. Steuer et al.   CANCER

Synthesis and evaluation of 2-anilinopyrimidines bearing 3-aminopropamides as potential epidermal growth factor receptor inhibitors

(2014) Chun Han et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a Potent and Selective EGFR Inhibitor (AZD9291) of Both Sensitizing and T790M Resistance Mutations That Spares the Wild Type Form of the Receptor

(2014) M. Raymond V. Finlay et al.   JOURNAL OF MEDICINAL CHEMISTRY

AZD9291, an Irreversible EGFR TKI, Overcomes T790M-Mediated Resistance to EGFR Inhibitors in Lung Cancer

(2014) D. A. E. Cross et al.   Cancer Discovery

Afatinib: First Global Approval

(2013) Rosselle T. Dungo et al.   DRUGS

Discovery of a Mutant-Selective Covalent Inhibitor of EGFR that Overcomes T790M-Mediated Resistance in NSCLC

(2013) A. O. Walter et al.   Cancer Discovery

Phase I Study of Lapatinib in Combination With Chemoradiation in Patients With Locally Advanced Squamous Cell Carcinoma of the Head and Neck

(2009) Kevin J. Harrington et al.   JOURNAL OF CLINICAL ONCOLOGY

Novel mutant-selective EGFR kinase inhibitors against EGFR T790M

(2009) Wenjun Zhou et al.   NATURE

Synthesis of new ribosylated Asn building blocks as useful tools for glycopeptide and glycoprotein synthesis

(2009) M. Angeles Bonache et al.   TETRAHEDRON LETTERS