Discovery of a series of 1, 2, 3-triazole-containing erlotinib derivatives with potent anti-tumor activities against non-small cell lung cancer

G Sun, L Mao, W Deng, S Xu, J Zhao, J Yang… - Frontiers in …, 2022 - frontiersin.org
Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) are emerging at
the vanguard of therapy for non-small-cell lung cancer (NSCLC) patients with EGFR …

Design, synthesis, and antitumor activity of erlotinib derivatives

L Mao, ZZ Wang, Q Wu, X Chen, JX Yang… - Frontiers in …, 2022 - frontiersin.org
Nineteen erlotinib derivatives bearing different 1, 2, 3-triazole moieties were designed,
synthesized, and evaluated for their potential against different cancer cell lines. The …

Discovery of EGFR tyrosine kinase inhibitors for cancer treatment

P Mahalapbutr, T Rungrotmongkol - Frontiers in Drug Discovery, 2024 - frontiersin.org
Tyrosine kinase inhibitors (TKIs) targeting the epidermal growth factor receptor (EGFR) have
long been established as conventional approaches for the treatment of non-small cell lung …

Design, synthesis, and biological evaluation of diphenyl ether substituted quinazolin-4-amine derivatives as potent EGFRL858R/T790M/C797S inhibitors

D Dou, X Zhang, J Wang, G Wumaier, Y Qiao… - European Journal of …, 2024 - Elsevier
Epidermal growth factor receptor (EGFR) is a validated target for non-small-cell lung cancer
(NSCLC). However, the treatment for EGFR-C797S mutation induced by third-generation …

[HTML][HTML] Appraisal and synthesis of novel indole-thiazole derivatives as epidermal growth factor receptor tyrosine kinase (EGFR-TK) inhibitors against resistance …

SV Tiwari, DN Pansare, DK Lokwani, SV Bhandari… - Results in …, 2024 - Elsevier
For the treatment of NSCLC one of the promising strategies is targeted inhibition of EGFR
and its mutants. In this research work, we tend to epitomize design, synthesis, in-vitro …

Design and Synthesis of New Hydantoin Acetanilide Derivatives as Anti-NSCLC Targeting EGFRL858R/T790M Mutations

MA Hassanin, M Mustafa, MAS Abourehab… - Pharmaceuticals, 2022 - mdpi.com
Epidermal Growth Factor Receptor (EGFR), its wild type and mutations L858R/T790M, is
overexpressed in non-small cell lung cancer (NSCLC) patients and is considered an …

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 …

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 …

Design, synthesis and biological evaluation of structurally new 4-indolyl quinazoline derivatives as highly potent, selective and orally bioavailable EGFR inhibitors

P He, L Du, Q Dai, G Li, B Yu, L Chang - Bioorganic Chemistry, 2024 - Elsevier
Targeting the epidermal growth factor receptor (EGFR) has been recognized as an effective
strategy for treating non-small-cell lung cancer (NSCLC). Although several representative …

A New Series of Indeno[1,2-c]pyrazoles as EGFR TK Inhibitors for NSCLC Therapy

A Özdemir, H Ciftci, B Sever, H Tateishi, M Otsuka… - Molecules, 2022 - mdpi.com
Non-small cell lung cancer (NSCLC) is the leading cause of cancer-related death
throughout the world. Due to the shortcomings of traditional chemotherapy, targeted …