Discovery of new [1, 4] dioxino [2, 3-f] quinazoline-based inhibitors of EGFR including the T790M/L858R mutant

X Qin, Z Li, L Yang, P Liu, L Hu, C Zeng… - Bioorganic & Medicinal …, 2016 - Elsevier
… ) values of twenty-one compounds against EGFR wt were less than 50 nM, and those of six
EGFR mutations L858R and delE746_A750, which account for 90% of all EGFR mutations in …

Discovery of novel 9-heterocyclyl substituted 9H-purines as L858R/T790M/C797S mutant EGFR tyrosine kinase inhibitors

H Lei, S Fan, H Zhang, YJ Liu, YY Hei, JJ Zhang… - European journal of …, 2020 - Elsevier
… Besides, Ding group found that compound 12 potently inhibited EGFR C797S mutated
as HBA in this study, and compound D9 was a potent promising EGFR L858 R/T790 M/C797S …

Discovery of novel potent covalent inhibitor-based EGFR degrader with excellent in vivo efficacy

S Shi, Y Du, L Huang, J Cui, J Niu, Y Xu, Q Zhu - Bioorganic Chemistry, 2022 - Elsevier
… or mutation Epidermal growth factor receptor (EGFR). The … of EGFR mutations are either
EGFR exon 19 deletion mutation (… compounds could selectively induce degradation of EGFR

A method of high-throughput functional evaluation of EGFR gene variants of unknown significance in cancer

S Kohsaka, M Nagano, T Ueno, Y Suehara… - Science translational …, 2017 - science.org
… (indicated at top) were treated with either DMSO or EGFR … expressing single or compound
EGFR mutations (indicated at … TKI sensitivity of EGFR compound mutants using the MANO …

Gefitinib, an effective treatment option for patients with pulmonary enteric adenocarcinoma harboring compound EGFR L858R and A871G mutation

Y Cui, J Liang, X Kang, M Liu, Q Zhang… - Investigational New …, 2023 - Springer
… combined with other mutations. To the … EGFR L858R + A871G compound mutation achieving
a 5-year progression-free survival (PFS) following postoperative treatment with the EGFR-…

[HTML][HTML] Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity

CH Yun, TJ Boggon, Y Li, MS Woo, H Greulich… - Cancer cell, 2007 - cell.com
… the structure of the wild-type EGFR kinase and the L858R and G719S mutants in complex
with inhibitors including gefitinib, AEE788, the staurosporine compound AFN941, and the ATP …

Design and synthesis of quinazolinones as EGFR inhibitors to overcome EGFR resistance obstacle

HM Patel, R Pawara, A Ansari, M Noolvi… - Bioorganic & medicinal …, 2017 - Elsevier
… inhibitory of the compounds against cancer cell lines with low level of EGFR expression was
… The cancer cell lines A549 express low levels of EGFR (WT EGFR and k-Ras mutation) and …

… approach with Biological Evaluation of Substituted Quinoline derivatives as small molecule L858R/T790M/C797S triple mutant EGFR inhibitors targeting resistance in …

KS Karnik, AP Sarkate, SV Tiwari, R Azad… - Bioorganic …, 2021 - Elsevier
… To appraise the potency for EGFR inhibitory activity, synthesized compounds 5(ap) were
tested against HCC827 cell line, harboring an EGFR-activating mutation (EGFR Del E746-A750…

Investigation of novel compounds via in silico approaches of EGFR inhibitors as anticancer agents

B Türkmenoğlu - Journal of the Indian Chemical Society, 2022 - Elsevier
… of non-small cell lung cancer patients with mutated EGFR and marginal in EGFR tumors [22]. …
idea of designing compounds with interactions at the active binding site of EGFR that could …

Novel EGFR inhibitors against resistant L858R/T790M/C797S mutant for intervention of non-small cell lung cancer

X Wang, Z Qin, W Qiu, K Xu, Y Bai, B Zeng, Y Ma… - European Journal of …, 2024 - Elsevier
… a novel compound 11eg as a potent EGFR C797S inhibitor. … To verify whether the selected
compounds exhibiting better … different EGFR mutants, including PC-9 expressing EGFR L858R…