Discovery of thiapyran-pyrimidine derivatives as potential EGFR inhibitors

Z Xiao, C Chu, L Zhou, Z Zhou, Q Zhang, F Yang… - Bioorganic & Medicinal …, 2020 - Elsevier
… representative EGFR inhibitors from the first generation to the third generation with EGFR
T790M kinase (Fig. … The first generation of EGFR-TKIs are mainly 4-phenylaminoquinazoline …

[HTML][HTML] Synthesis, anticancer activity and docking studies of pyrazoline and pyrimidine derivatives as potential epidermal growth factor receptor (EGFR) inhibitors

M Al-Anazi, M Khairuddean, BO Al-Najjar… - Arabian Journal of …, 2022 - Elsevier
… ) depends on several pyrimidine derivatives including adenine, guanine, … EGFR inhibitors
as anticancer agents (Al-Anazi et al., 2018; Al-Anazi et al., 2021), compounds with pyrimidine

An assessment of EGFR and HER2 inhibitors with structure activity relationship of fused pyrimidine derivatives for breast cancer: a brief review

PS Dhiwar, GS Purawarga Matada, R Pal… - Journal of …, 2024 - Taylor & Francis
EGFR and HER2 inhibitors which contain pyrimidine ring. The compilation of data from
sub-class of pyrimidine derivatives … in designing of EGFR and HER2 inhibitors. The summary of …

Design, synthesis and antitumor activity of novel thiophene-pyrimidine derivatives as EGFR inhibitors overcoming T790M and L858R/T790M mutations

Z Xiao, Z Zhou, C Chu, Q Zhang, L Zhou, Z Yang… - European Journal of …, 2020 - Elsevier
… We designed and synthesized five series of thiophene-pyrimidine derivatives in this paper.
The most promising compound showed superior activity against A549, A431 and Hela, with …

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
… 2,3-d]pyrimidine derivatives as an EGFR and HER2 tyrosine kinase inhibitors. All the
synthesized compounds were evaluated in vitro for their inhibitory activities against EGFR WT ; and …

Design, synthesis and antitumor activity of novel pyrazolo [3, 4-d] pyrimidine derivatives as EGFR-TK inhibitors

MA Abdelgawad, RB Bakr, OA Alkhoja… - Bioorganic chemistry, 2016 - Elsevier
… Docking studies into ATP binding site of EGFR protein tyrosine kinase were performed to …
(EGFR-TK) was evaluated. Results indicated the ability of the target compounds to inhibit EGFR

Discovery of anilino-furo [2, 3-d] pyrimidine derivatives as dual inhibitors of EGFR/HER2 tyrosine kinase and their anticancer activity

M Hossam, DS Lasheen, NSM Ismail, A Esmat… - European Journal of …, 2018 - Elsevier
… types, EGFR (… ]pyrimidine derivatives was designed, synthesized and biologically evaluated.
Modification of the solvent accessible 5-position side chain greatly affected the in-vitro EGFR

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
… to develop effective EGFR-TKIs, two series of 1H-pyrazolo[3,4-d]pyrimidine derivatives were
… inhibitory activities against EGFR WT . Compounds 15 b , 15 j , and 18 d potently inhibited …

Pyrimidine-based EGFR TK inhibitors in targeted cancer therapy

A Ayati, S Moghimi, M Toolabi, A Foroumadi - European Journal of …, 2021 - Elsevier
… especially pyrimidine containing … inhibitors of EGFR tyrosine kinase (TK) domain [17].
Clinical data have shown the significant influence of pyrimidine derivatives as EGFR TK inhibitors

Design, synthesis and evaluation of new pyrimidine derivatives as EGFRC797S tyrosine kinase inhibitors

YZ Mao, XX Xi, HY Zhao, YL Zhang… - Bioorganic & Medicinal …, 2023 - Elsevier
… Our group also reported that 8-phenylthio-9H-purine, 28 9-heterocyclyl substituted 9H-purines
29 and pyrido[3,4-d]pyrimidine derivatives 30 as new EGFR L858R/T790M/C797S …