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

Author(s): Xin-Hua Liu , Jun Li , Fan-Rong Wu , Bao-An Song , Pinaki S. Bhadury , Lei Shi .

Journal Name: Medicinal Chemistry

Volume 7 , Issue 6 , 2011

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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.

Keywords: 4H-chromen, dihydropyrazole, molecular docking, anticancer activity, 3-(2-(3-methyl-5-substituted-phenyl-4,5-dihydropyrazol-1-yl), 4H-chromen-4-one derivatives, telomerase with IC50, probable binding model, pharmaceutically, chromosomal integrity

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Article Details

Year: 2011
Page: [605 - 610]
Pages: 6
DOI: 10.2174/157340611797928442
Price: $58

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