Design, Synthesis, and Anticancer Activity Evaluation of Hybrids of Azoles and Barbituric Acids
| Author | Hong-Juan Liu | en |
| Author | Xing Huang | en |
| Author | Qing-Kun Shen | en |
| Author | Hao Deng | en |
| Author | Zhiyong Li | en |
| Author | Zhe-Shan Quan | en |
| Issued Date | 2021-04-30 | en |
| Abstract | In order to find new drugs with potent antiproliferative effect, a series of novel barbituric acid derivatives containing azoles at the C-5 position were designed, synthesized, and evaluated for antiproliferative activity against three human cancer cell lines (BEL-7402, MCF-7, and HCT-116) using MTT assay. Several of the synthesized compounds exhibited potent antiproliferative effects. The most promising compound was 5-((1-(4-(trifluoromethyl)phenyl)-1H-1,2,3-triazol-4-yl) methylene)pyrimidine-2,4,6(1H,3H,5H)-trione (3s), which showed considerably high antiproliferative activity in the BEL-7402 cell line, with a half-maximal inhibitory concentration of 4.02 µM and 20.45-fold higher selectivity for BEL-7402 cells than for normal L02 cells. The apoptosis experiment showed that compound 3s induced apoptosis and cell necrosis in a concentration-dependent manner and exert its anti-proliferative activity. Therefore, compound 3s exhibited better therapeutic activity and specificity compared with the positive control 5-fluorouracil. | en |
| DOI | https://doi.org/10.22037/ijpr.2020.113547.14363 | en |
| Keyword | Barbituric acid | en |
| Keyword | 1 | en |
| Keyword | 2 | en |
| Keyword | 3-triazoles | en |
| Keyword | Anticancer | en |
| Keyword | MTT assay | en |
| Keyword | Cell apoptosis | en |
| Publisher | Brieflands | en |
| Title | Design, Synthesis, and Anticancer Activity Evaluation of Hybrids of Azoles and Barbituric Acids | en |
| Type | Original Article | en |
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