☆ 4.2 Article

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

LETTERS IN DRUG DESIGN & DISCOVERY (2010)

期刊

LETTERS IN DRUG DESIGN & DISCOVERY

卷 7, 期 9, 页码 640-643

出版社

BENTHAM SCIENCE PUBL LTD

DOI: 10.2174/157018010792929540

关键词

Coumarin; Dihydropyrazole; Molecular Docking; Antitumor Agent

类别

Chemistry, Medicinal

资金

National Natural Science Foundation of China [20902003]
University Natural Science, Anhui Province [KJ2009A011Z]

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Protocol

Reagent

摘要

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.

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