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

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 H-1 NMR and C-13 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 mu g/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 mu M, respectively. Docking simulation was performed to position compound 6cf into the telomerase (3DU6) active site to determine the probable binding model.