Novel 2-(5-Aryl-4, 5-dihydropyrazol-1-yl) thiazol-4-one as EGFR inhibitors: synthesis, biological assessment and molecular docking insights
… 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 …
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
… 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 …
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 …
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 …
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 inhibitors … EGFR kinases in
nanomolar range. We have demonstrated by Western blot analysis that compound 10 inhibits EGFR …
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 …
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 …
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 …
… 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 …
… 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 …
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, …
molecular dynamics simulation. … for inhibitor activity prediction against FGFR4 and EGFR. Then, …
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