EGFR mutations in non-small cell lung cancer: an audit from West China Hospital
Y Tang, W Wang, K Zheng, L Jiang, Y Zou… - Expert Review of …, 2016 - Taylor & Francis
… represents the largest EGFR mutation survey based on … EGFR mutations in NSCLC seen
in Asian patients, and also unravels the combinatorial nature of rare compound EGFR mutations…
in Asian patients, and also unravels the combinatorial nature of rare compound EGFR mutations…
Toward discovery of mutant EGFR inhibitors; Design, synthesis and in vitro biological evaluation of potent 4-arylamino-6-ureido and thioureido-quinazoline derivatives
S Mowafy, A Galanis, ZM Doctor, RM Paranal… - Bioorganic & medicinal …, 2016 - Elsevier
… Overexpression and mutations of EGFR and ErbB2 have been observed in various human
… study, we concluded that compounds targeting dual inhibition of EGFR and ErbB2 afforded …
… study, we concluded that compounds targeting dual inhibition of EGFR and ErbB2 afforded …
[HTML][HTML] Detection of rare and novel EGFR mutations in NSCLC patients: Implications for treatment-decision
AC Sousa, C Silveira, A Janeiro, S Malveiro… - Lung Cancer, 2020 - Elsevier
… We further found six new single mutations and seven previously unreported compound …
to identify rare mutations. Our results add to the inventory of known EGFR mutations, thus …
to identify rare mutations. Our results add to the inventory of known EGFR mutations, thus …
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
… Among them, Compound 6a showed good inhibitory activity against EGFR mutant cells with
an IC 50 value of 0.0022 ± 0.001 μM and was approximately 1730-fold less potent against …
an IC 50 value of 0.0022 ± 0.001 μM and was approximately 1730-fold less potent against …
Structural investigations of T854A mutation in EGFR and identification of novel inhibitors using structure activity relationships
… We report two novel compounds having high predicted inhibitory activity to EGFR TK …
polymorphism in tyrosine kinase domain of EGFR. The compounds reported in this study can be …
polymorphism in tyrosine kinase domain of EGFR. The compounds reported in this study can be …
Discovery of novel allosteric EGFR L858R inhibitors for the treatment of non-small-cell lung cancer as a single agent or in combination with osimertinib
U Obst-Sander, A Ricci, B Kuhn, T Friess… - Journal of medicinal …, 2022 - ACS Publications
… of the compounds to inhibit phosphorylation of EGFR L858R/… the mutated proteins and
the stability of the compounds in … at the EGFR L858R/T790M/C797S mutation was retained, …
the stability of the compounds in … at the EGFR L858R/T790M/C797S mutation was retained, …
… evaluation of new series of hexahydroquinoline and fused quinoline derivatives as potent inhibitors of wild-type EGFR and mutant EGFR (L858R and T790M)
MA Shaheen, AA El-Emam, NS El-Gohary - Bioorganic Chemistry, 2020 - Elsevier
… new drugs targeting EGFR L858R and EGFR T790M mutants to overcome resistance to first…
of the potent antitumor compound 7d to EGFR WT , EGFR L858R , EGFR T790M and JAK3, …
of the potent antitumor compound 7d to EGFR WT , EGFR L858R , EGFR T790M and JAK3, …
Discovery of selective irreversible inhibitors for EGFR-T790M
… mutation relative to wild-type EGFR were discovered by library screening. A representative
compound … covalent compounds because effective targeting of the T790M EGFR mutant with …
compound … covalent compounds because effective targeting of the T790M EGFR mutant with …
Discovery of BLU-945, a reversible, potent, and wild-type-sparing next-generation EGFR mutant inhibitor for treatment-resistant non-small-cell lung cancer
MS Eno, JD Brubaker, JE Campbell… - Journal of medicinal …, 2022 - ACS Publications
… to decreased potency on EGFR mutants of interest. Turning our … compound library, we
identified compound 4 with moderate EGFR mutant potency but excellent selectivity over WT-EGFR…
identified compound 4 with moderate EGFR mutant potency but excellent selectivity over WT-EGFR…
Start selective and rigidify: the discovery path toward a next generation of EGFR tyrosine kinase inhibitors
H Engelhardt, D Böse, M Petronczki… - Journal of medicinal …, 2019 - ACS Publications
… compound to exhibit a next generation EGFR TKI profile, wt-sparing, capable of inhibiting
complex EGFR mutations … , including a triple cis mutation in the EGFR del19 background. Key …
complex EGFR mutations … , including a triple cis mutation in the EGFR del19 background. Key …