標題: Synthesis and Evaluation of Aminothiazole-Paeonol Derivatives as Potential Anticancer Agents
作者: Tsai, Chia-Ying
Kapoor, Mohit
Huang, Ying-Pei
Lin, Hui-Hsien
Liang, Yu-Chuan
Lin, Yu-Ling
Huang, Su-Chin
Liao, Wei-Neng
Chen, Jen-Kun
Huang, Jer-Shing
Hsu, Ming-Hua
生物科技學系
生物資訊研究中心
Department of Biological Science and Technology
Center for Bioinformatics Research
關鍵字: paeonol;2-aminothiazole;anti-cancer;sulfonate;adenocarcenoma
公開日期: 1-Feb-2016
摘要: 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.
URI: http://dx.doi.org/10.3390/molecules21020145
http://hdl.handle.net/11536/133537
ISSN: 1420-3049
DOI: 10.3390/molecules21020145
期刊: MOLECULES
Volume: 21
Issue: 2
起始頁: 0
結束頁: 0
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