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 …

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 …

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 …

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 …

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 …

Discovery of 5-(methylthio) pyrimidine derivatives as L858R/T790M mutant selective epidermal growth factor receptor (EGFR) inhibitors

Q Xiao, R Qu, D Gao, Q Yan, L Tong, W Zhang… - Bioorganic & Medicinal …, 2016 - Elsevier
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) …

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 …

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 …

New thieno[2,3‐d]pyrimidine derivatives as EGFRWT and EGFRT790M inhibitors: Design, synthesis, antiproliferative activities, docking studies, ADMET, toxicity, MD …

EA Sobh, MA Dahab, EB Elkaeed… - Journal of …, 2024 - Wiley Online Library
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 …

Fused bicyclic and tricyclic pyrimidine compounds as tyrosine kinase inhibitors

HP Hsieh, SM Coumar, TA Hsu, WH Lin… - US Patent …, 2013 - Google Patents
BACKGROUND Protein kinases play important roles in cellular signal path ways that
regulate various cell functions such as differentia tion, proliferation, migration, and …