Design, synthesis and evaluation of new pyrimidine derivatives as EGFRC797S tyrosine kinase inhibitors
YZ Mao, XX Xi, HY Zhao, YL Zhang… - Bioorganic & Medicinal …, 2023 - Elsevier
The clinical use of epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs)
in the treatment of non-small cell lung cancer was limited by the drug resistance caused by …
in the treatment of non-small cell lung cancer was limited by the drug resistance caused by …
Discovery of novel 9-heterocyclyl substituted 9H-purines as L858R/T790M/C797S mutant EGFR tyrosine kinase inhibitors
Abstract Targeting L858R/T790M/C797S mutant EGFR is a major challenge in the new-
generation EGFR tyrosine kinase inhibitors development for conquering drug resistant …
generation EGFR tyrosine kinase inhibitors development for conquering drug resistant …
Design, synthesis and biological evaluation of 2-phenylaminopyrimidine derivatives as EGFR inhibitors
C Tang, J Wang, D Wang, H Wang, S Cui, T Xiao… - Bioorganic & Medicinal …, 2024 - Elsevier
In the treatment of non-small cell lung cancer (NSCLC), acquired drug resistance is a major
factor that affects the efficacy of third-generation epidermal growth factor receptor (EGFR) …
factor that affects the efficacy of third-generation epidermal growth factor receptor (EGFR) …
Novel anilinopyrimidine derivatives as potential EGFRT790M/C797S Inhibitors: Design, Synthesis, biological activity study
Y Guo, B Gao, P Gao, L Fang, S Gou - Bioorganic & Medicinal Chemistry, 2022 - Elsevier
Abstract EGFR T790M/C797S is an important target for the development of new generation
of EGFR kinase inhibitors without drug resistance. In this work, a series of anilinopyrimidine …
of EGFR kinase inhibitors without drug resistance. In this work, a series of anilinopyrimidine …
Design, synthesis and biological evaluation of novel 2, 4-diaryl pyrimidine derivatives as selective EGFRL858R/T790M inhibitors
J Li, B An, X Song, Q Zhang, C Chen, S Wei… - European Journal of …, 2021 - Elsevier
Lung cancer is the leading cause of cancer deaths. It has been demonstrated that epidermal
growth factor receptor tyrosine kinase inhibitors (EGFR-TKI) are efficacious in patients with …
growth factor receptor tyrosine kinase inhibitors (EGFR-TKI) are efficacious in patients with …
XHL11, a novel selective EGFR inhibitor, overcomes EGFRT790M-mediated resistance in non-small cell lung cancer
Y Li, QL Yu, TF Li, YN Xiao, L Zhang, QY Zhang… - European Journal of …, 2021 - Elsevier
The first-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors
(TKIs), gefitinib and erlotinib significantly improved the therapeutic effect in non–small cell …
(TKIs), gefitinib and erlotinib significantly improved the therapeutic effect in non–small cell …
Design, synthesis and biological evaluation of aminopyrimidine derivatives bearing a 4, 5, 6, 7-tetrahydrothieno [3, 2-c] pyridine as potent EGFR inhibitors
Y Li, Y Chang, J Fu, R Ding, L Zhang, T Liang… - European Journal of …, 2021 - Elsevier
To resolve the problem of drug resistance caused by epidermal growth factor receptor
(EGFR) mutations in non-small cell lung cancer, we used the principle of collocation to …
(EGFR) mutations in non-small cell lung cancer, we used the principle of collocation to …
2-Oxo-3, 4-dihydropyrimido [4, 5-d] pyrimidines as new reversible inhibitors of EGFR C797S (Cys797 to Ser797) mutant
Extensive structure-activity relationships (SARs) study of JND3229 was conducted to yield a
series of new reversible 2-oxo-3, 4-dihydropyrimido [4, 5-d] pyrimidine privileged scaffold as …
series of new reversible 2-oxo-3, 4-dihydropyrimido [4, 5-d] pyrimidine privileged scaffold as …
Design, synthesis and evaluation of the Brigatinib analogues as potent inhibitors against tertiary EGFR mutants (EGFRdel19/T790M/C797S and EGFRL858R/T790M …
H Fang, Y Wu, Q Xiao, D He, T Zhou, W Liu… - Bioorganic & Medicinal …, 2022 - Elsevier
Although epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) have
demonstrated encouraging clinical outcomes for patients with EGFR-mutated non-small cell …
demonstrated encouraging clinical outcomes for patients with EGFR-mutated non-small cell …
Design, synthesis and antitumor activity of 4-arylamine substituted pyrimidine derivatives as noncovalent EGFR inhibitors overcoming C797S mutation
Y Zuo, Z Long, R Li, Y Le, S Zhang, H He… - European Journal of …, 2024 - Elsevier
Clinical researches have shown that epidermal growth factor receptor (EGFR) is a key target
for treatment of non-small cell lung cancer (NSCLC). Many EGFR inhibitors were …
for treatment of non-small cell lung cancer (NSCLC). Many EGFR inhibitors were …
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