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Title: Quinazolinones as allosteric fourth-generation EGFR inhibitors for the treatment of NSCLC

Journal Article · · Bioorg. Med. Chem. Lett.

Research Organization:
Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Sponsoring Organization:
DOE - Office Of Science; FOREIGN
Journal Information:
Bioorg. Med. Chem. Lett., Vol. 68
Country of Publication:
United States

References (15)

Properties of FDA-approved small molecule protein kinase inhibitors: A 2021 update journal March 2021
Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases journal January 2021
A review on progression of epidermal growth factor receptor (EGFR) inhibitors as an efficient approach in cancer targeted therapy journal June 2020
The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP journal January 2008
Structure- and Reactivity-Based Development of Covalent Inhibitors of the Activating and Gatekeeper Mutant Forms of the Epidermal Growth Factor Receptor (EGFR) journal August 2013
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 journal October 2014
Mechanisms of osimertinib resistance and emerging treatment options journal September 2020
New Promise and Opportunities for Allosteric Kinase Inhibitors journal April 2020
Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors journal May 2016
Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor journal May 2019
Complex Crystal Structures of EGFR with Third-Generation Kinase Inhibitors and Simultaneously Bound Allosteric Ligands journal November 2020
An allosteric inhibitor against the therapy-resistant mutant forms of EGFR in non-small cell lung cancer journal April 2022
Allosteric Inhibitor TREA-0236 Containing Non-hydrolysable Quinazoline-4-one for EGFR T790M/C797S Mutants Inhibition: Allosteric Inhibitor TREA-0236 Containing Non-hydrolysable Quinazoline-4-one for EGFR T790M/C797S Mutants Inhibition journal June 2018
Finding the perfect spot for fluorine: Improving potency up to 40-fold during a rational fluorine scan of a Bruton’s Tyrosine Kinase (BTK) inhibitor scaffold journal January 2015
Synthesis of 3-Substituted-4(3 H )-quinazolinones via HATU-Mediated Coupling of 4-Hydroxyquinazolines with Amines journal February 2009

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