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Molecules 2016, 21(2), 145; doi:10.3390/molecules21020145

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

1
Nuclear Science & Technology Development Center, National Tsing Hua University, Hsinchu 30013, Taiwan
2
Department of Chemistry, National Tsing Hua University, Hsinchu 30013, Taiwan
3
Division of Radiotherapy, Department of Oncology, Taipei Veterans General Hospital, Taipei 11217, Taiwan
4
Agricultural Biotechnology Research Center, Academia Sinica, Taipei 115, Taiwan
5
Department of Biological Science and Technology, National Chiao Tung University, Hsinchu 30010, Taiwan
6
Center for Bioinformatics Research, National Chiao Tung University, Hsinchu 30010, Taiwan
7
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)
View Full-Text   |   Download PDF [649 KB, uploaded 26 January 2016]   |  

Abstract

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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MDPI and ACS Style

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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