Design, synthesis, and biological evaluation of pyrido[2,3-d]pyrimidine and thieno[2,3-d]pyrimidine derivatives as novel EGFRL858R/T790M inhibitors
J Fu, J Yu, X Zhang, Y Chang, H Fan… - Journal of Enzyme …, 2023 - Taylor & Francis
EGFR mutations have been identified in 20,000 reported NSCLC (non-small cell lung
cancer) samples, and exon 19 deletions and L858R mutations at position 21, known as …
cancer) samples, and exon 19 deletions and L858R mutations at position 21, known as …
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 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 …
Rational design and synthesis of 2,4‐dichloro‐6‐methyl pyrimidine derivatives as potential selective EGFRT790M/L858R inhibitors for the treatment of non‐small cell …
L Duan, C Chu, X Huang, H Yao, J Wen… - Archiv der …, 2024 - Wiley Online Library
Many patients with non‐small cell lung cancer (NSCLC) initially benefit from epidermal
growth factor receptor (EGFR) targeted therapy. Unfortunately, varying degrees of resistance …
growth factor receptor (EGFR) targeted therapy. Unfortunately, varying degrees of resistance …
Novel third-generation pyrimidines-based EGFR tyrosine kinase inhibitors targeting EGFR T790M mutation in advanced non-small cell lung cancer
B An, J Liu, Y Fan, W Nie, C Yang, H Yao, W Li… - Bioorganic …, 2022 - Elsevier
The critical T790M secondary mutation in epidermal growth-factor receptor (EGFR) mediates
resistance to first-and second-generation EGFR tyrosine kinase inhibitors. Herein, we …
resistance to first-and second-generation EGFR tyrosine kinase inhibitors. Herein, we …
Discovery of 5-(methylthio) pyrimidine derivatives as L858R/T790M mutant selective epidermal growth factor receptor (EGFR) inhibitors
To overcome the drug-resistance of first generation EGFR inhibitors and the nonselective
toxicities of second generation inhibitors among NSCLC patients, a series of 5-(methylthio) …
toxicities of second generation inhibitors among NSCLC patients, a series of 5-(methylthio) …
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 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 …
New thieno[2,3‐d]pyrimidine derivatives as EGFRWT and EGFRT790M inhibitors: Design, synthesis, antiproliferative activities, docking studies, ADMET, toxicity, MD …
Abstract A series of thieno [2, 3‐d] pyrimidines were designed and synthesized as epidermal
growth factor receptor (EGFR) inhibitors. These compounds were tested for their ability to …
growth factor receptor (EGFR) inhibitors. These compounds were tested for their ability to …
Fused bicyclic and tricyclic pyrimidine compounds as tyrosine kinase inhibitors
BACKGROUND Protein kinases play important roles in cellular signal path ways that
regulate various cell functions such as differentia tion, proliferation, migration, and …
regulate various cell functions such as differentia tion, proliferation, migration, and …
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