Novel 2-(5-Aryl-4, 5-dihydropyrazol-1-yl) thiazol-4-one as EGFR inhibitors: synthesis, biological assessment and molecular docking insights

T Al-Warhi, AM El Kerdawy, MA Said… - Drug Design …, 2023 - Taylor & Francis
… are in agreement with the expected outcome of EGFR inhibition. Finally, the molecular docking
of 7g and 7m in the active site of EGFR revealed a common binding pattern similar to that …

[HTML][HTML] Globally approved EGFR inhibitors: Insights into their syntheses, target kinases, biological activities, receptor interactions, and metabolism

MAS Abourehab, AM Alqahtani, BGM Youssif… - Molecules, 2021 - mdpi.com
… the EGFR inhibitors discussed in this review. … EGFR inhibitors which target EGFR with high
selectivity such as gefitinib; (2) dual EGFR inhibitors such as lapatinib which can target EGFR

Design, synthesis and biological evaluation of a series of dianilinopyrimidines as EGFR inhibitors

L Yan, Q Wang, L Liu, Y Le - Journal of Enzyme Inhibition and …, 2022 - Taylor & Francis
EGFR inhibitors. All the target compounds were tested for inhibitory effects against wild type
EGFR (EGFR … compound 4c could closely interact with EGFR. Generally, compound 4c was …

Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors

AM Srour, NS Ahmed, SS Abd El-Karim… - Bioorganic & Medicinal …, 2020 - Elsevier
EGFR inhibitors. The derivatives that exhibited promising EGFR inhibitory effects were further
assessed … The candidate which revealed characteristic EGFR inhibition and showed potent …

Discovery and biological evaluation of novel dual EGFR/c-Met inhibitors

B Szokol, P Gyulavári, I Kurkó, F Baska… - ACS Medicinal …, 2014 - ACS Publications
… In the present study we have identified dual EGFR/c-Met inhibitorsEGFR kinases in
nanomolar range. We have demonstrated by Western blot analysis that compound 10 inhibits EGFR

Novel sulfonyl thiazolyl-hydrazone derivatives as EGFR inhibitors: Design, synthesis, biological evaluation and molecular docking studies

TA Farghaly, EMH Abbas, AM Al-Soliemy, R Sabour… - Bioorganic …, 2022 - Elsevier
… as EGFR inhibitors affecting both MCF-7 and HepG2 cancer cell lines using MTT assay.
Newly synthesized compounds were assessed for their potential inhibition against EGFR. Most …

Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting EGFR

J Wu, W Chen, G Xia, J Zhang, J Shao… - ACS Medicinal …, 2013 - ACS Publications
… from irreversible EGFR inhibitors is a … EGFR inhibitor 9n did not display obvious inhibition
on the growth of A549, SW620, and K562 cancer cells, all of which have low levels of EGFR

[HTML][HTML] … , in vitro biological assessment and molecular modeling insights for novel 3-(naphthalen-1-yl)-4, 5-dihydropyrazoles as anticancer agents with potential EGFR …

WM Eldehna, MA El Hassab, ZM Elsayed, T Al-Warhi… - Scientific reports, 2022 - nature.com
… features of EGFR inhibitors are required for maximum affinity against the EGFR ATP binding
… many anticancer molecules through the inhibition of diverse RTKs including EGFR 22,23 . In …

[HTML][HTML] Targeted inhibitors of EGFR: structure, biology, biomarkers, and clinical applications

N Shaban, D Kamashev, A Emelianova, A Buzdin - Cells, 2023 - mdpi.com
… However, we found no indications that this drug can work better than other EGFR inhibitors.
Instead, results of a phase III study showed that patients with advanced NSCLC after prior …

Discovery of dual FGFR4 and EGFR inhibitors by machine learning and biological evaluation

X Chen, W Xie, Y Yang, Y Hua, GM Xing… - Journal of Chemical …, 2020 - ACS Publications
… -target inhibitors against both FGFR4 and EGFR by artificial … of dual-target inhibitors by
molecular dynamics simulation. … for inhibitor activity prediction against FGFR4 and EGFR. Then, …