Design, synthesis and biological evaluation of potent epidermal growth factor receptor tyrosine kinase (EGFR-TK) inhibitors against resistance mutation for lung …

C Wang, X Wang, X Wang, B Tian, S Zhang, T Wang… - Bioorganic …, 2024 - Elsevier
In this study, we identified a newly synthesized compound 7o with potent inhibition on EGFR
primary mutants (L858R, Del19) and drug-resistant mutant T790M with nanomolar IC 50 …

[PDF][PDF] Phase I study of HM61713, a novel epidermal growth factor receptor (EGFR) mutant selective inhibitor, in non-small cell lung cancer (NSCLC) patients having …

DW Kim, SW Kim, TM Kim, SH Lee, CM Choi… - J Thorac …, 2013 - old.hanmi.co.kr
Background▪ NSCLC patients having an activating EGFR mutation initially responded well to
EGFR TKI but most of them experienced progressive disease due to various resistance …

Design, synthesis, and biological evaluation of novel quinoline derivatives as small molecule mutant EGFR inhibitors targeting resistance in NSCLC: In vitro screening …

RA Kardile, AP Sarkate, DK Lokwani, SV Tiwari… - European Journal of …, 2023 - Elsevier
Here in, we report the design, synthesis and in vitro anticancer activity of a novel series of 24
quinoline analogues of substituted amide and sulphonamide derivatives. The anticancer …

Abstract C189: CO-1686, an orally available, mutant-selective inhibitor of the epidermal growth factor receptor (EGFR), causes tumor shrinkage in non-small cell lung …

AO Walter, R Tjin, H Haringsma, K Lin… - Molecular Cancer …, 2011 - AACR
Introduction: Non-small cell lung cancer (NSCLC) patients with activating EGFR mutations
initially respond well to EGFR tyrosine kinase inhibitors. However, clinical efficacy is limited …

Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors

N Hoogenboom, D Demont, E de Zwart… - Bioorganic & Medicinal …, 2021 - Elsevier
Epidermal growth factor receptor (EGFR) inhibitors have clinical utility in the treatment of non-
small cell lung cancer (NSCLC) patients. Despite encouraging clinical efficacy with these …

Abstract LB-100: Discovery of HM61713 as an orally available and mutant EGFR selective inhibitor

KO Lee, MY Cha, M Kim, JY Song, JH Lee, YH Kim… - Cancer Research, 2014 - AACR
Introduction: Activating mutations of EGFR are well known as oncogenic driver mutations in
lung adenocarcinoma. Currently, EGFR TKIs including Gefitinib and Erlotinib are used as …

Computational and Synthetic approach with Biological Evaluation of Substituted Quinoline derivatives as small molecule L858R/T790M/C797S triple mutant EGFR …

KS Karnik, AP Sarkate, SV Tiwari, R Azad… - Bioorganic …, 2021 - Elsevier
New substituted quinoline derivatives were designed and synthesized via a five-step
modified Suzuki coupling reaction. A comparative molecular docking study was carried out …

A novel scaffold for EGFR inhibition: Introducing N-(3-(3-phenylureido)quinoxalin-6-yl) acrylamide derivatives

DN do Amaral, J Lategahn, HH Fokoue… - Scientific reports, 2019 - nature.com
Clinical data acquired over the last decade on non-small cell lung cancer (NSCLC)
treatment with small molecular weight Epidermal Growth Factor Receptor (EGFR) inhibitors …

A sulfonyl fluoride derivative inhibits EGFRL858R/T790M/C797S by covalent modification of the catalytic lysine

F Ferlenghi, L Scalvini, F Vacondio, R Castelli… - European Journal of …, 2021 - Elsevier
The emergence of the C797S mutation in EGFR is a frequent mechanism of resistance to
osimertinib in the treatment of non-small cell lung cancer (NSCLC). In the present work, we …

The new N2, N4-diphenylpyridine-2, 4-diamine deuterated derivatives as EGFR inhibitors to overcome C797S-mediated resistance

J Liu, W Nie, H Nie, H Yao, Y Ren, L Cao, J Qiu… - Bioorganic …, 2024 - Elsevier
A series of new deuterated and non-deuterated N 2, N 4-diphenylpyridine− 2, 4-diamine
derivatives were synthesized and evaluated as EGFR C797S-mediated resistance …