Coumarin-furo[2,3-<i>d</i>]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% in

SUBMITTER: Wang T 

PROVIDER: S-EPMC11110736 | biostudies-literature | 2024 May

REPOSITORIES: biostudies-literature