Design, synthesis and biological evaluation of aminopyrimidine derivatives bearing a 4,5,6,7-tetrahydrothieno [3,2-c]pyridine as potent EGFR inhibitors

Design, synthesis and antitumor activity of novel thiophene-pyrimidine derivatives as EGFR inhibitors overcoming T790M and L858R/T790M mutations

(2020) Zhen Xiao et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of selective EGFR modulator to inhibit L858R/T790M double mutants bearing a N- 9-Diphenyl-9 H -purin-2-amine scaffold

(2018) Jinxing Hu et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Design, synthesis and biological evaluation of novel 7-amino-[1,2,4]triazolo[4,3-f]pteridinone, and 7-aminotetrazolo[1,5-f]pteridinone derivative as potent antitumor agents

(2018) Yunlei Hou et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants

(2017) Haoyang Zhang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Olmutinib: First Global Approval

(2016) Esther S. Kim   DRUGS

Association Between Plasma Genotyping and Outcomes of Treatment With Osimertinib (AZD9291) in Advanced Non–Small-Cell Lung Cancer

(2016) Geoffrey R. Oxnard et al.   JOURNAL OF CLINICAL ONCOLOGY

Third-generation inhibitors targeting EGFR T790M mutation in advanced non-small cell lung cancer

(2016) Shuhang Wang et al.   Journal of Hematology & Oncology

Global cancer statistics, 2012

(2015) Lindsey A. Torre et al.   CA-A CANCER JOURNAL FOR CLINICIANS

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

EGFR gene-mutation status correlated with therapeutic decision making in lung adenocarcinoma

(2015) Yaoyao Ren et al.   OncoTargets and Therapy

RB loss in resistant EGFR mutant lung adenocarcinomas that transform to small-cell lung cancer

(2015) Matthew J. Niederst et al.   Nature Communications

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

Acquired resistance to TKIs in solid tumours: learning from lung cancer

(2014) D. Ross Camidge et al.   Nature Reviews Clinical Oncology

The role of ligand efficiency metrics in drug discovery

(2014) Andrew L. Hopkins et al.   NATURE REVIEWS DRUG DISCOVERY

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

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

Structure-based design and optimization of 2-aminothiazole-4-carboxamide as a new class of CHK1 inhibitors

(2013) Xiaohua Huang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

A novel amalgamation of 1,2,3-triazoles, piperidines and thieno pyridine rings and evaluation of their antifungal activity

(2013) Sunil N. Darandale et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

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

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

Neratinib, an Irreversible Pan-ErbB Receptor Tyrosine Kinase Inhibitor: Results of a Phase II Trial in Patients With Advanced Non–Small-Cell Lung Cancer

(2010) Lecia V. Sequist et al.   JOURNAL OF CLINICAL ONCOLOGY

Emerging role of gefitinib in the treatment of non-small-cell lung cancer (NSCLC)

(2010) Marcello Tiseo   Drug Design Development and Therapy

Rapid assessment of a novel series of selective CB2 agonists using parallel synthesis protocols: A Lipophilic Efficiency (LipE) analysis

(2009) Thomas Ryckmans et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Novel mutant-selective EGFR kinase inhibitors against EGFR T790M

(2009) Wenjun Zhou et al.   NATURE

EGFR Antagonists in Cancer Treatment

(2008) Fortunato Ciardiello et al.   NEW ENGLAND JOURNAL OF MEDICINE

BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models

(2008) D Li et al.   ONCOGENE