New quinazoline-N-4-fluorophenyl derivatives as potential anticancer agents: Discovery of a promising dual EGFR/VEGFR-2 inhibitor

This research is dedicated to synthesizing a new group of quinazoline-N-4-fluorophenyl 4a–d structures and evaluating their anticancer efficacy across multiple cancer cell lines. The molecular design of these derivatives was based on the structural features required for dual inhibition of VEGFR-2 and EGFR. The new derivatives were structurally characterised by NMR analyses. Cytotoxicity was assessed in this study against various cancerous cell strains. Among these, the top three products were further assessed for their capacity to block the enzymatic activity of (VEGFR-2) and (EGFR). Product 4b , in particular, exhibited a strong cytotoxic profile, with IC 50 values of 68.2 ± 1.54 nM against EGFR and 189 ± 5.66 nM against VEGFR-2. Molecular docking studies demonstrated that compound 4b effectively interacts with the active sites of both VEGFR-2 and EGFR, potentially influencing its action pathway as a powerful inhibitor.

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Publication Details

Journal
Journal of King Saud University - Science
Published
2024-11-04
DOI
https://doi.org/10.1016/j.jksus.2024.103518
Citations
1
Primary Topic
Quinazolinone synthesis and applications
Type
article
Field-Weighted Citation Impact
0.25

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article

New quinazoline-N-4-fluorophenyl derivatives as potential anticancer agents: Discovery of a promising dual EGFR/VEGFR-2 inhibitor

Mohammed H. Geesi
1 citations
Journal of King Saud University - Science
Quinazolinone synthesis and applications
0.25
article

New quinazoline-N-4-fluorophenyl derivatives as potential anticancer agents: Discovery of a promising dual EGFR/VEGFR-2 inhibitor

Mohammed H. Geesi
article en
1 citations

Abstract

This research is dedicated to synthesizing a new group of quinazoline-N-4-fluorophenyl 4a–d structures and evaluating their anticancer efficacy across multiple cancer cell lines. The molecular design of these derivatives was based on the structural features required for dual inhibition of VEGFR-2 and EGFR. The new derivatives were structurally characterised by NMR analyses. Cytotoxicity was assessed in this study against various cancerous cell strains. Among these, the top three products were further assessed for their capacity to block the enzymatic activity of (VEGFR-2) and (EGFR). Product 4b , in particular, exhibited a strong cytotoxic profile, with IC 50 values of 68.2 ± 1.54 nM against EGFR and 189 ± 5.66 nM against VEGFR-2. Molecular docking studies demonstrated that compound 4b effectively interacts with the active sites of both VEGFR-2 and EGFR, potentially influencing its action pathway as a powerful inhibitor.

Journal of King Saud University - ScienceVol. 36(11)
Prince Sattam Bin Abdulaziz University (SA)
Prince Sattam bin Abdulaziz University
Openalex Percentile: Top 47%
Quinazolinone synthesis and applications
0.25
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New quinazoline-N-4-fluorophenyl derivatives as potential anticancer agents: Discovery of a promising dual EGFR/VEGFR-2 inhibitor — Mohammed H. Geesi · Journal of King Saud University - Science (2024) | TGRS Research Map | TGRS