Synthesis and in vitro anticancer evaluation of some fused indazoles, quinazolines and quinolines as potential EGFR inhibitors

EA Abdelsalam, WA Zaghary, KM Amin… - Bioorganic …, 2019 - Elsevier
… The results were reported as 50% inhibitionEGFR inhibitory activity with IC 50 values
ranging from 0.13 to 3.50 μM. Compounds 15c and 19b were the most potent EGFR inhibitors in …

EGFR-targeted anti-cancer drugs in radiotherapy: preclinical evaluation of mechanisms

M Baumann, M Krause, E Dikomey, K Dittmann… - Radiotherapy and …, 2007 - Elsevier
EGFR inhibitors appear to be considerably different to those for application of EGFR inhibitors
… Therefore to further evaluate the efficacy and mechanisms of EGFR-inhibition in combined …

Development of pyridazine derivatives as potential EGFR inhibitors and apoptosis inducers: Design, synthesis, anticancer evaluation, and molecular modeling studies

MF Ahmed, EY Santali, EMM El-Deen, IA Naguib… - Bioorganic …, 2021 - Elsevier
… In addition, in vitro studies of the epidermal growth factor receptor (EGFR) inhibition showed
… IXg and IXn due to their significant EGFR inhibition. Flow cytometeric analysis indicated that …

Design, synthesis and anticancer evaluation of 1H-pyrazolo [3, 4-d] pyrimidine derivatives as potent EGFRWT and EGFRT790M inhibitors and apoptosis inducers

AA Gaber, AH Bayoumi, AM El-Morsy, FF Sherbiny… - Bioorganic …, 2018 - Elsevier
… The wide variety of modifications enabled us to study the SAR of these compounds as
effective anti-cancer agents with potential EGFR-TK inhibitory activity which is considered as a …

Dual target inhibitors based on EGFR: Promising anticancer agents for the treatment of cancers (2017-)

L Hu, M Fan, S Shi, X Song, F Wang, H He… - European Journal of …, 2022 - Elsevier
… In vitro anticancer activities were evaluated in the NCI-60 cellular assays across several
panels from leukemia, prostate, NSCLC, breast, colon and CNS cell lines, and the GI 50 values …

Design, synthesis and anticancer evaluation of thieno [2, 3-d] pyrimidine derivatives as dual EGFR/HER2 inhibitors and apoptosis inducers

SA Elmetwally, KF Saied, IH Eissa, EB Elkaeed - Bioorganic chemistry, 2019 - Elsevier
EGFR and HER2 tyrosine kinase inhibitors. All the synthesized compounds were evaluated
in vitro for their inhibitory activities against EGFR … IC 50 values against EGFR WT were tested …

New pyrimidine and pyrazole-based compounds as potential EGFR inhibitors: Synthesis, anticancer, antimicrobial evaluation and computational studies

IMM Othman, ZM Alamshany, NY Tashkandi… - Bioorganic …, 2021 - Elsevier
… Accordingly, there is still a great demand to develop new EGFR inhibitors with high
selectivity against the EGFR T790M and EGFR L858R mutation to overcome the undesirable …

Synthesis, anticancer activity and molecular modeling studies of 1, 2, 4-triazole derivatives as EGFR inhibitors

HAM El-Sherief, BGM Youssif, SNA Bukhari… - European journal of …, 2018 - Elsevier
… be evaluated for their anticancer activity and EGFR inhibition. According to our published
research [19], acylation on N-1 of 5-amino-1,2,4-triazoles enhanced their EGFR … the anticancer

Epidermal growth factor receptor tyrosine kinase inhibitors as anticancer agents

F Ciardiello - Drugs, 2000 - Springer
… these EGFR-TKIs… anticancer agents in preclinical models. ZD1839 (‘Iressa’), 1,2 an
anilinoquinazoline, is an orally active, selective EGFR-TKI which is currently under clinical evaluation

Novel 4-(2-arylidenehydrazineyl) thienopyrimidine derivatives as anticancer EGFR inhibitors: Design, synthesis, biological evaluation, kinome selectivity and in silico …

HA Elsebaie, EA El-Bastawissy, KM Elberembally… - Bioorganic …, 2023 - Elsevier
… that targeted EGFR inhibition is a potent … evaluated as EGFR-TK inhibitors, and the EGFR
inhibitors that are now on the market can be divided into first- through fourth-generation EGFR