Synthesis and Evaluation of Aminothiazole-Paeonol Derivatives as Potential Anticancer Agents
AbstractIn 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
Scifeed alert for new publicationsNever miss any articles matching your research from any publisher
- Get alerts for new papers matching your research
- Find out the new papers from selected authors
- Updated daily for 49'000+ journals and 6000+ publishers
- Define your Scifeed now
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.
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(2):145.Chicago/Turabian Style
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. 2016. "Synthesis and Evaluation of Aminothiazole-Paeonol Derivatives as Potential Anticancer Agents." Molecules 21, no. 2: 145.
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.