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 …
Design, synthesis and biological evaluation of potent EGFR kinase inhibitors against 19D/T790M/C797S mutation
Z Su, T Yang, J Wang, M Lai, L Tong, G Wumaier… - Bioorganic & Medicinal …, 2020 - Elsevier
The efficacy of EGFR inhibitors is frequently affected by acquired resistance. EGFR
19D/T790M/C797S mutation is one of the primary reasons for the emergence of resistance …
19D/T790M/C797S mutation is one of the primary reasons for the emergence of resistance …
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 …
Noncovalent EGFR T790M/L858R inhibitors based on diphenylpyrimidine scaffold: design, synthesis, and bioactivity evaluation for the treatment of NSCLC
L Chen, Y Zhang, L Tian, C Wang, T Deng… - European Journal of …, 2021 - Elsevier
A series of diphenylpyrimidine derivatives bearing a hydroxamic acid group was designed
and synthesized as noncovalent EGFR T790M/L858R inhibitors to improve the biological …
and synthesized as noncovalent EGFR T790M/L858R inhibitors to improve the biological …
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 …
Design, synthesis and biological evaluation of phosphoroxy quinazoline derivatives as potential EGFRT790M/C797S inhibitors
Y Guo, B Gao, P Gao, Y Wang, S Gou - Bioorganic & Medicinal Chemistry, 2023 - Elsevier
Owing to the urgency and importance of developing fourth-generation EGFR inhibitors that
can effectively overcome C797S site mutation in NSCLC, Brigatinib was used in this work as …
can effectively overcome C797S site mutation in NSCLC, Brigatinib was used in this work as …
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 …
The synthesis of 4-arylamido-2-arylaminoprimidines as potent EGFR T790M/L858R inhibitors for NSCLC
L Chen, F Chi, T Wang, N Wang, W Li, K Liu… - Bioorganic & Medicinal …, 2018 - Elsevier
Abstract A series of 4-arylamido-2-arylaminoprimidines bearing acrylamide pharmacophore
were synthesized as potent EGFR T790M/L858R inhibitors among which 9c (IC 50= 0.5872 …
were synthesized as potent EGFR T790M/L858R inhibitors among which 9c (IC 50= 0.5872 …
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 …
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