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

Gero, Thomas W.; Heppner, David E.; Beyett, Tyler S.; To, Ciric; Azevedo, Seth C.; Jang, Jaebong; Bunnell, Thomas; Feru, Frederic; Li, Zhengnian; Shin, Bo Hee; Soroko, Kara M.; Gokhale, Prafulla C.; Gray, Nathanael S.; Janne, Pasi A.; Eck, Michael J.; Scott, David A.

doi:10.1016/j.bmcl.2022.128718

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

Journal Article · Fri Jul 01 04:00:00 EDT 2022 · Bioorg. Med. Chem. Lett.

DOI:https://doi.org/10.1016/j.bmcl.2022.128718· OSTI ID:1867470

Gero, Thomas W.; Heppner, David E.; Beyett, Tyler S.; To, Ciric; Azevedo, Seth C.; Jang, Jaebong; Bunnell, Thomas; Feru, Frederic; Li, Zhengnian; Shin, Bo Hee; Soroko, Kara M.; Gokhale, Prafulla C.; Gray, Nathanael S.; Janne, Pasi A.; Eck, Michael J.; Scott, David A.

Research Organization:: Advanced Photon Source (APS), Argonne National Laboratory (ANL), Argonne, IL (US)

Sponsoring Organization:: DOE - Office Of Science; FOREIGN

OSTI ID:: 1867470

Journal Information:: Bioorg. Med. Chem. Lett., Journal Name: Bioorg. Med. Chem. Lett. Vol. 68

Country of Publication:: United States

Language:: ENGLISH

References (15)

Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases Xie, Zhouling; Yang, Xiaoxiao; Duan, Yajun Journal of Medicinal Chemistry, Vol. 64, Issue 3 https://doi.org/10.1021/acs.jmedchem.0c01511	journal	January 2021
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 Lee, Seoyoung; Kim, Jiwon; Duggirala, Krishna Babu Bulletin of the Korean Chemical Society, Vol. 39, Issue 7 https://doi.org/10.1002/bkcs.11491	journal	June 2018
Structure- and Reactivity-Based Development of Covalent Inhibitors of the Activating and Gatekeeper Mutant Forms of the Epidermal Growth Factor Receptor (EGFR) Ward, Richard A.; Anderton, Mark J.; Ashton, Susan Journal of Medicinal Chemistry, Vol. 56, Issue 17 https://doi.org/10.1021/jm400822z	journal	August 2013
Mechanisms of osimertinib resistance and emerging treatment options Schmid, Sabine; Li, Janice J. N.; Leighl, Natasha B. Lung Cancer, Vol. 147 https://doi.org/10.1016/j.lungcan.2020.07.014	journal	September 2020
Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors Jia, Yong; Yun, Cai-Hong; Park, Eunyoung Nature, Vol. 534, Issue 7605 https://doi.org/10.1038/nature17960	journal	May 2016
The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP Yun, C. -H.; Mengwasser, K. E.; Toms, A. V. Proceedings of the National Academy of Sciences, Vol. 105, Issue 6 https://doi.org/10.1073/pnas.0709662105	journal	January 2008
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 Finlay, M. Raymond V.; Anderton, Mark; Ashton, Susan Journal of Medicinal Chemistry, Vol. 57, Issue 20 https://doi.org/10.1021/jm500973a	journal	October 2014
A review on progression of epidermal growth factor receptor (EGFR) inhibitors as an efficient approach in cancer targeted therapy Ayati, Adileh; Moghimi, Setareh; Salarinejad, Somayeh Bioorganic Chemistry, Vol. 99 https://doi.org/10.1016/j.bioorg.2020.103811	journal	June 2020
Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor To, Ciric; Jang, Jaebong; Chen, Ting Cancer Discovery, Vol. 9, Issue 7 https://doi.org/10.1158/2159-8290.CD-18-0903	journal	May 2019
Complex Crystal Structures of EGFR with Third-Generation Kinase Inhibitors and Simultaneously Bound Allosteric Ligands Niggenaber, Janina; Heyden, Leonie; Grabe, Tobias ACS Medicinal Chemistry Letters, Vol. 11, Issue 12 https://doi.org/10.1021/acsmedchemlett.0c00472	journal	November 2020
Synthesis of 3-Substituted-4(3 H )-quinazolinones via HATU-Mediated Coupling of 4-Hydroxyquinazolines with Amines Xiao, Zili; Yang, Michael G.; Li, Peng Organic Letters, Vol. 11, Issue 6 https://doi.org/10.1021/ol802946p	journal	February 2009
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 Lou, Yan; Sweeney, Zachary K.; Kuglstatter, Andreas Bioorganic & Medicinal Chemistry Letters, Vol. 25, Issue 2 https://doi.org/10.1016/j.bmcl.2014.11.030	journal	January 2015
New Promise and Opportunities for Allosteric Kinase Inhibitors Lu, Xiaoyun; Smaill, Jeff B.; Ding, Ke Angewandte Chemie International Edition, Vol. 59, Issue 33 https://doi.org/10.1002/anie.201914525	journal	April 2020
Properties of FDA-approved small molecule protein kinase inhibitors: A 2021 update Roskoski, Robert Pharmacological Research, Vol. 165 https://doi.org/10.1016/j.phrs.2021.105463	journal	March 2021
An allosteric inhibitor against the therapy-resistant mutant forms of EGFR in non-small cell lung cancer To, Ciric; Beyett, Tyler S.; Jang, Jaebong Nature Cancer, Vol. 3, Issue 4 https://doi.org/10.1038/s43018-022-00351-8	journal	April 2022

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