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 …
T790M kinase (Fig. … The first generation of EGFR-TKIs are mainly 4-phenylaminoquinazoline …
Pyrimidine-based EGFR TK inhibitors in targeted cancer therapy
… 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 …
Clinical data have shown the significant influence of pyrimidine derivatives as EGFR TK inhibitors …
[HTML][HTML] Synthesis, anticancer activity and docking studies of pyrazoline and pyrimidine derivatives as potential epidermal growth factor receptor (EGFR) inhibitors
… ) 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 …
as anticancer agents (Al-Anazi et al., 2018; Al-Anazi et al., 2021), compounds with pyrimidine …
Design, synthesis and antitumor activity of novel thiophene-pyrimidine derivatives as EGFR inhibitors overcoming T790M and L858R/T790M mutations
… 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 …
The most promising compound showed superior activity against A549, A431 and Hela, with …
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
… As seen from its binding mode with EGFR T790M , the aniline pyrimidine core of WZ4002
formed a crucial bidentate hydrogen bond with the “hinge” residue Met793 (Figure 3A). The …
formed a crucial bidentate hydrogen bond with the “hinge” residue Met793 (Figure 3A). The …
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 …
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
… EGFR overexpression has been implicated in numerous … Therefore, EGFR inhibition
represents a rational approach for … A number of small molecule EGFR kinase inhibitors had been …
represents a rational approach for … A number of small molecule EGFR kinase inhibitors had been …
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…
Modification of the solvent accessible 5-position side chain greatly affected the in-vitro EGFR…
Discovery of new 1H-pyrazolo[3,4-d]pyrimidine derivatives as anticancer agents targeting EGFRWT and EGFRT790M
… ]pyrimidine derivative with anti-EGFR activityCitation 38 . Furthermore, our team synthesised
1H-pyrazolo[3,4-d]pyrimidine derivative (compound VII) as EGFR inhibitor… and mutant EGFR…
1H-pyrazolo[3,4-d]pyrimidine derivative (compound VII) as EGFR inhibitor… and mutant EGFR…
Discovery of new pyrimidine-5-carbonitrile derivatives as anticancer agents targeting EGFR WT and EGFR T790M
… of pyrimidine-5-carbonitrile derivatives having the essential pharmacophoric features of EGFR…
Next, we tested whether the EGFR WT inhibition can lead to cell death. To confirm this, the …
Next, we tested whether the EGFR WT inhibition can lead to cell death. To confirm this, the …
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