Novel 3-(1-(2-(2,7a-dihydrobenzo[d]thiazol-2-ylthio)acetyl)-5-substituted- phenyl-4,5-dihydro-1H-pyrazol-3-yl)-Coumarins: Synthesis and anticancer activity
LETTERS IN DRUG DESIGN & DISCOVERY(2012)
Abstract
Seven novel 3-(1-(2-(2,7a-dihydrobenzo[d] thiazol-2-ylthio) acetyl)-5-substituted-phenyl-4,5-dihydro-1H-pyrazol- 3-yl)-2H-chromen-2-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 4g exhibited potentially high activity against human gastric cancer cell SGC-7901 with IC50 value of 6.99 +/- 1.10 mu g/mL. Docking simulation was performed to position compound 4g into the telomerase (3DU6) active site to determine the probable binding model.
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Key words
Coumarins,Dihydropyrazole,Molecular Docking,Anticancer activity
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