Pyrimidine derivatives as EGFR tyrosine kinase inhibitors in non‐small‐cell lung cancer: A comprehensive review

A Kizhakkedath Ratheesh… - Chemical Biology & …, 2022 - Wiley Online Library
EGFR‐positive non‐small‐cell lung cancer (NSCLC) due to primary mutation (EGFR DEL19
& L858R) has been recognized as a crucial mediator of tumor progression. This led to the …

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 …

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 …

Design, synthesis and pharmacological evaluation of N4, N6-disubstituted pyrimidine-4, 6-diamine derivatives as potent EGFR inhibitors in non-small cell lung cancer

Y Zhang, H Lv, L Luo, Y Xu, Y Pan, Y Wang… - European Journal of …, 2018 - Elsevier
Image 2 A novel series of 4, 6-disubstituted pyrimidines derivatives were designed,
synthesized, and evaluated as epidermal growth factor receptor (EGFR) inhibitors for non …

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 …

[HTML][HTML] Next-Generation EGFR Tyrosine Kinase Inhibitors for Treating EGFR-Mutant Lung Cancer beyond First Line

I Sullivan, D Planchard - Frontiers in medicine, 2017 - frontiersin.org
Tyrosine kinase inhibitors (TKIs) against the human epidermal growth factor receptor
(EGFR) are now standard treatment in the clinic for patients with advanced EGFR mutant …

Clinical activity and safety of HM61713, an EGFR-mutant selective inhibitor, in advanced non-small cell lung cancer (NSCLC) patients (pts) with EGFR mutations who …

DW Kim, DH Lee, JH Kang, K Park, JY Han, JS Lee… - 2014 - ascopubs.org
8011 Background: HM61713 is a novel, oral, selective inhibitor for EGFR mutations
including both activating mutations and T790M, but not EGFR wild-type. This phase 1 trial …

The role of EGFR tyrosine kinase inhibitors in the first-line treatment of advanced non small cell lung cancer patients harboring EGFR mutation

A Sgambato, F Casaluce, P Maione… - Current medicinal …, 2012 - ingentaconnect.com
Lung cancer continues to be the leading cause of cancer death worldwide. Among lung
cancers, 80% are classified as nonsmall-cell lung cancer (NSCLC) and are mostly …

Emerging agents and new mutations in EGFR-mutant lung cancer

D Ayeni, K Politi, SB Goldberg - Clinical Cancer Research, 2015 - AACR
Third-generation mutant-specific EGFR tyrosine kinase inhibitors are showing robust clinical
activity, particularly in lung cancers harboring the EGFRT790M mutation, yet acquired …

HM61713, an EGFR-mutant selective inhibitor

DW Kim - Annals of Oncology, 2015 - Elsevier
ABSTRACT EGFR tyrosine kinase inhibitors (TKIs) are effective for EGFR mutation positive
non-small cell lung cancer (NSCLC) patients. However, acquired resistance occurs in most …