化学
蛇床子素
立体化学
天然产物
碳-13核磁共振
细胞毒性
组合化学
酰胺
癌细胞系
质子核磁共振
细胞培养
体外
齐墩果酸
癌细胞
癌症
有机化学
生物化学
内科学
替代医学
病理
生物
医学
遗传学
作者
Diego Rodríguez-Hernández,Antônio J. Demuner,Luiz C. A. Barbosa,Lucie Heller,René Csük
标识
DOI:10.1016/j.ejmech.2016.03.018
摘要
A series of novel aryl-1H-1,2,3-triazol-4-yl methylester and amide derivatives of the natural product hederagenin was synthesized aiming to develop new antitumor agents, using Huisgen 1,3-dipolar cycloaddition reactions, with yields between 35% and 95%. The structures of all derivatives (2–31) were confirmed by MS, IR, 1H NMR and 13C NMR spectroscopic data. The cytotoxic activities of all compounds were screened against a panel of six human cancer cell lines using SRB assay. It was found that most of the compounds displayed higher levels of antitumor activities as compared to parent hederagenin. Compounds 4, 8 and 15 were the most potent against all human cancer cell lines. Furthermore, compound 11 was the most cytotoxic against cell HT29 showing EC50 = 1.6 μM and a selectivity index of 5.4.
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