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Seven novel 3-(1-(2-(2,7a-dihydrobenzo[d]thiazol-2-ylthio)acetyl)-5-substituted-phenyl-4,5-dihydro-1Hpyrazol- 3-yl)-2H-chromen-2-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 4g exhibited potentially high activity against human gastric cancer cell SGC-7901 with IC50 value of 6.99±1.10 μg/mL. Docking simulation was performed to position compound 4g into the telomerase (3DU6) active site to determine the probable binding model.