Issue 5, 2024

Coumarin–furo[2,3-d]pyrimidone hybrid molecules targeting human liver cancer cells: synthesis, anticancer effect, EGFR inhibition and molecular docking studies

Abstract

The design, synthesis and investigation of antitumor activities of some coumarin–furo[2,3-d]pyrimidone hybrid molecules are reported. In vitro, HepG2 cells were used to investigate the cytotoxicity of 6a–n and 10a–n. The results demonstrated that coupling a furopyrimidone scaffold with coumarin through a hydrazide linker can effectively improve their synergistic anticancer activity. The coumarin–furo[2,3-d]pyrimidone combination 10a exhibited significant inhibitory activity against HepG2 cells with IC50 = 7.72 ± 1.56 μM, which is better than those of gefitinib and sorafenib. It is worth mentioning that the coumarin–furo[2,3-d]pyrimidone combination 10a showed excellent inhibition of the EGFR enzymatic activity with IC50 = 1.53 μM and 90% inhibition at 10 μM concentration. In silico investigation predicts the possibility of direct binding between the new coumarin–furo[2,3-d]pyrimidone hybrid molecules and the EGFR. The results suggest that coumarin–furo[2,3-d]pyrimidone hybrid molecules are potential antitumor agents targeting human liver cancer cells.

Graphical abstract: Coumarin–furo[2,3-d]pyrimidone hybrid molecules targeting human liver cancer cells: synthesis, anticancer effect, EGFR inhibition and molecular docking studies

Supplementary files

Article information

Article type
Research Article
Submitted
29 Nov 2023
Accepted
16 Mar 2024
First published
19 Mar 2024

RSC Med. Chem., 2024,15, 1565-1577

Coumarin–furo[2,3-d]pyrimidone hybrid molecules targeting human liver cancer cells: synthesis, anticancer effect, EGFR inhibition and molecular docking studies

T. Wang, Y. Gao, F. Wu, L. Luo, J. Ma and Y. Hu, RSC Med. Chem., 2024, 15, 1565 DOI: 10.1039/D3MD00668A

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