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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Novel 3-(1-(2-(2,7a-dihydrobenzo[d]thiazol-2-ylthio)acetyl)-5-substitutedphenyl-4,5-dihydro-1H-pyrazol-3-yl)-Coumarins: Synthesis and Anticancer Activity

Author(s): Xian-Hai Lv, Xiu-Li Zhang, Xin-Hua Liu and Lei Shi

Volume 9, Issue 2, 2012

Page: [199 - 203] Pages: 5

DOI: 10.2174/157018012799079743

Price: $65

Abstract

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.

Keywords: Coumarins, Dihydropyrazole, Molecular Docking, Anticancer activity, Telomerase, chromosomal integrity, 3DU6, gastric SGC-7901, dihydropyrazole heterocycle, Claisen-Schmidt, mother liquor, column chromatography, Cytotoxic Assay, Colorless crystals


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