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-acetyl-5-(substituted-phenyl)-4,5-dihydro-1H-pyrazol-3-yl)-7-fluoro-2H-chromen-2-one Derivatives: Synthesis and Anticancer Activity

Author(s): Zheng-Yu Cai, Yang Yang, Xin-Hua Liu, Xing-Bao Qi.

Abstract:

A series of novel coumarin derivatives containing 4,5-dihydropyrazole moiety as potential telomerase inhibitors were synthesized. The bioassay tests showed that compound 3b exhibited potentially high activity against human gastric cancer cell SGC-7901 with IC50 value was 2.98±0.16. Docking simulation was performed to position compound 3b into the telomerase (3DU6) active site to determine the probable binding model. The result shows that some coumarin containing 4,5-dihydropyrazole moiety can combine well with the telomerase active site and may have use as potential telomerase inhibitors.

Keywords: Coumarin, Dihydropyrazole, Molecular Docking, Antitumor Agent, Anticancer activity, Telomerase inhibitiors, Immortality, Ageing makes, Age-associated disorders, Human gastric cancer, Human liver cancer, Cytostatic properties, Cytotoxic activity, Mammalian cancer, Small bioactive molecule, CB1 antagonist, Docking simulation, Telomerase 3DU6, XT-4 binocular microscope, Pulse Fourier-transform NMR spectrometer, Analytical reagent-grade, Human gastric cell, Potent inhibitor, Telomerase, Binding mode, ATP binding site

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Article Details

VOLUME: 7
ISSUE: 9
Year: 2010
Page: [640 - 643]
Pages: 4
DOI: 10.2174/157018010792929540
Price: $58