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Molecules 2016, 21(2), 145;

Synthesis and Evaluation of Aminothiazole-Paeonol Derivatives as Potential Anticancer Agents

Nuclear Science & Technology Development Center, National Tsing Hua University, Hsinchu 30013, Taiwan
Department of Chemistry, National Tsing Hua University, Hsinchu 30013, Taiwan
Division of Radiotherapy, Department of Oncology, Taipei Veterans General Hospital, Taipei 11217, Taiwan
Agricultural Biotechnology Research Center, Academia Sinica, Taipei 115, Taiwan
Department of Biological Science and Technology, National Chiao Tung University, Hsinchu 30010, Taiwan
Center for Bioinformatics Research, National Chiao Tung University, Hsinchu 30010, Taiwan
Institute of Biomedical Engineering and Nanomedicine, National Health Research Institutes, Miaoli 35053, Taiwan
These authors contributed equally to this work.
Authors to whom correspondence should be addressed.
Academic Editors: Jean Jacques Vanden Eynde and Annie Mayence
Received: 20 November 2015 / Revised: 11 January 2016 / Accepted: 20 January 2016 / Published: 26 January 2016
(This article belongs to the Section Medicinal Chemistry)
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In this study, novel aminothiazole-paeonol derivatives were synthesized and characterized using 1H-NMR, 13C-NMR, IR, mass spectroscopy, and high performance liquid chromatography. All the new synthesized compounds were evaluated according to their anticancer effect on seven cancer cell lines. The experimental results indicated that these compounds possess high anticancer potential regarding human gastric adenocarcinoma (AGS cells) and human colorectal adenocarcinoma (HT-29 cells). Among these compounds, N-[4-(2-hydroxy-4-methoxyphenyl)thiazol-2-yl]-4-methoxybenzenesulfonamide (13c) had the most potent inhibitory activity, with IC50 values of 4.0 µM to AGS, 4.4 µM to HT-29 cells and 5.8 µM to HeLa cells. The 4-fluoro-N-[4-(2-hydroxy-4-methoxyphenyl)thiazol-2-yl]benzenesulfonamide (13d) was the second potent compound, showing IC50 values of 7.2, 11.2 and 13.8 µM to AGS , HT-29 and HeLa cells, respectively. These compounds are superior to 5-fluorouracil (5-FU) for relatively higher potency against AGS and HT-29 human cancer cell lines along with lower cytotoxicity to fibroblasts. Novel aminothiazole-paeonol derivatives in this work might be a series of promising lead compounds to develop anticancer agents for treating gastrointestinal adenocarcinoma. View Full-Text
Keywords: paeonol; 2-aminothiazole; anti-cancer; sulfonate; adenocarcenoma paeonol; 2-aminothiazole; anti-cancer; sulfonate; adenocarcenoma

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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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Tsai, C.-Y.; Kapoor, M.; Huang, Y.-P.; Lin, H.-H.; Liang, Y.-C.; Lin, Y.-L.; Huang, S.-C.; Liao, W.-N.; Chen, J.-K.; Huang, J.-S.; Hsu, M.-H. Synthesis and Evaluation of Aminothiazole-Paeonol Derivatives as Potential Anticancer Agents. Molecules 2016, 21, 145.

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