https://scholars.lib.ntu.edu.tw/handle/123456789/639668
標題: | Design, synthesis, and anti-cancer evaluation of C-14 arylcarbamate derivatives of andrographolide | 作者: | Yang, Tzu-Ching Chiang, Yun-Jou Chiang, Po-Yu Chen, Han-Yu Zhuang, Kai-Ru Wang, Yu-Chia Lin, Chao-Hsiung LEE-CHIANG LO Fu, Shu-Ling |
關鍵字: | Andrographolide; Anticancer; Covalent; Cytotoxicity; Electrophilic; Natural product | 公開日期: | 15-一月-2024 | 卷: | 98 | 來源出版物: | Bioorganic & medicinal chemistry | 摘要: | In this study, we explored a concise and mild synthetic route to produce novel C-14 arylcarbamate derivatives of andrographolide, a known anti-inflammatory and anticancer natural product. Upon assessing their anti-cancer efficacy against pancreatic ductal adenocarcinoma (PDAC) cells, some derivatives showed stronger cytotoxicity against PANC-1 cells than andrographolide. In addition, we demonstrated one derivative, compound 3m, effectively reduced the expression of oncogenic p53 mutant proteins (p53R273H and p53R248W), proliferation, and migration in PDAC lines, PANC-1 and MIA PaCa-2. Accordingly, the novel derivative holds promise as an anti-cancer agent against pancreatic cancer. In summary, our study broadens the derivative library of andrographolide and develops an arylcarbamate derivative of andrographolide with promising anticancer activity against PDAC. |
URI: | https://scholars.lib.ntu.edu.tw/handle/123456789/639668 | ISSN: | 09680896 | DOI: | 10.1016/j.bmc.2023.117582 |
顯示於: | 化學系 |
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