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

Chia Ying Tsai, Mohit Kapoor, Ying Pei Huang, Hui Hsien Lin, Yu Chuan Liang, Yu-Ling Lin, Su Chin Huang, Wei Neng Liao, Jen Kun Chen, Jer Shing Huang, Ming Hua Hsu

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In this study, novel aminothiazole-paeonol derivatives were synthesized and characterized using H-1-NMR, C-13-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 mu M to AGS, 4.4 mu M to HT-29 cells and 5.8 mu M 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 mu M 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.
Original languageEnglish
StatePublished - Feb 2016


  • paeonol; 2-aminothiazole; anti-cancer; sulfonate; adenocarcenoma

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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. (2016). Synthesis and Evaluation of Aminothiazole-Paeonol Derivatives as Potential Anticancer Agents. Molecules.