Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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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, Lei Shi.

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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Article Details

VOLUME: 9
ISSUE: 2
Year: 2012
Page: [199 - 203]
Pages: 5
DOI: 10.2174/157018012799079743
Price: $58