Novel 3-(2-(3-methyl-5-substituted-phenyl-4,5-dihydropyrazol-1-yl)-2-oxoethoxy)-2-substituted-phenyl-4H-chromen-4-one: synthesis and anticancer activity
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Updated: May 25, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Xin-Hua Liu1, Jun Li, Fan-Rong Wu
1School of Pharmacy, Anhui Medical University, Hefei, 230032, PR China.
Abstract:
Ten novel 3-(2-(3-methyl-5-substituted-phenyl-4,5-dihydropyrazol-1-yl)-2-oxo-ethoxy)-2-substituted-phenyl-4H-chromen-4-one derivatives were synthesized and characterized by 1H NMR and 13 C NMR. All of the compounds have been screened for their anticancer activity. The bioassay tests show that compound 6af exhibited potentially high activity against human gastric cancer cell SGC-7901 with IC50 value of 4.01±0.97 μg/mL. Also, the title compounds were assayed for telomerase inhibition. The results show that compounds 6cf, 6af can strongly inhibit telomerase with IC50 values of 4.89±0.11 and 5.02±0.91 μM, respectively. Docking simulation was performed to position compound 6cf into the telomerase (3DU6) active site to determine the probable binding model.
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