A Series of 2,4(1H,3H)-Quinazolinedione Derivatives: Synthesis and Biological Evaluation as Potential Anticancer Agents

Author(s): Hulya Akgun, Demet Us Yilmaz, Rengul Cetin Atalay, Damla Gozen

Journal Name: Letters in Drug Design & Discovery

Volume 13 , Issue 1 , 2016

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Graphical Abstract:


A series of 6,7-disubstituted-3-{2-[4-(substituted)piperazin-1-yl]-2-oxoethyl}quinazoline- 2,4(1H,3H)-dione derivatives (7-34) were synthesized and their structures were elucidated on the basis of analytical and spectral (UV, IR, 1H-NMR, 13C-NMR and MS) data. These synthesized compounds were evaluated for their in vitro cytotoxicities against a panel of three human cancer cell lines. According to the cytotoxicity screening results, 3-{2-[4-(4-chlorobenzyl)piperazin-1-yl]-2-oxoethyl} quinazoline-2,4(1H,3H)-dione (7) presented the highest activity against HUH-7, MCF-7 and HCT-116 cell line with the IC50 values of 2.5, 6.8 and 4.9 µM, respectively.

Keywords: Quinazoline, quinazoline-2, 4(1H, 3H)-dione, piperazine, cytotoxicity, anticancer, sulforhodamine B method.

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Article Details

Year: 2016
Published on: 29 May, 2015
Page: [64 - 76]
Pages: 13
DOI: 10.2174/1570180812666150529204909

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