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Molecules 2017, 22(7), 1154;

Synthesis and Evaluation of New Quinoxaline Derivatives of Dehydroabietic Acid as Potential Antitumor Agents

Jiangsu Key Lab of Biomass-Based Green Fuels and Chemicals, College of Chemical Engineering, Nanjing Forestry University, Nanjing 210037, China
The State Key Lab of Pharmaceutical Biotechnology, School of Life Sciences, Nanjing University, Nanjing 210093, China
The two authors contributed equally to this work.
Author to whom correspondence should be addressed.
Received: 14 April 2017 / Accepted: 4 July 2017 / Published: 11 July 2017
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A series of new quinoxaline derivatives of dehydroabietic acid (DAA) were designed and synthesized as potential antitumor agents. Their structures were characterized by IR, 1H-NMR, 13C-NMR, and MS spectra and elemental analyses. All the new compounds were screened for their in vitro antiproliferative activities against three human cancer cell lines (MCF-7, SMMC-7721 and HeLa) and noncancerous human hepatocyte cells (LO2). A cytotoxic assay manifested that compound 4b showed the most potent cytotoxic activity against the three cancer cell lines, with IC50 values of 1.78 ± 0.36, 0.72 ± 0.09 and 1.08 ± 0.12 μM, respectively, and a substantially lower cytotoxicity to LO2 cells (IC50: 11.09 ± 0.57 μM). Moreover, the cell cycle analysis suggested that compound 4b caused cell cycle arrest of SMMC-7721 cells at the G0/G1 phase. In a Hoechst 33258 staining assay, compound 4b caused considerable morphological changes of the nuclei of SMMC-7721 cells, correlated with cell apoptosis. In addition, an Annexin V-FITC/PI dual staining assay confirmed that compound 4b could induce the apoptosis of SMMC-7721 cells in a dose-dependent manner. View Full-Text
Keywords: dehydroabietic acid; quinoxaline; antitumor activity; cell cycle; apoptosis dehydroabietic acid; quinoxaline; antitumor activity; cell cycle; apoptosis

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Gu, W.; Wang, S.; Jin, X.; Zhang, Y.; Hua, D.; Miao, T.; Tao, X.; Wang, S. Synthesis and Evaluation of New Quinoxaline Derivatives of Dehydroabietic Acid as Potential Antitumor Agents. Molecules 2017, 22, 1154.

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