Synthesis and Cytotoxicity in Vitro of N‐Aryl‐4‐(tert‐butyl)‐5‐(1H‐1,2,4‐triazol‐1‐yl)thiazol‐2‐amine |
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Authors: | Jiao Ye Meng‐Wu Xiao Xuan‐Qing Xie Shen‐Yi Qiu Ming‐Chong Dai Wan Li Fang Shen Ai‐Xi Hu |
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Affiliation: | 1. College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, China, Tel: +86 0731‐88822286;2. Fax: +86 0731‐88713642 |
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Abstract: | A series of novel N‐aryl‐4‐(tert‐butyl)‐5‐(1H‐1,2,4‐triazol‐1‐yl)thiazol‐2‐amines synthesized in a green way. H2O2‐NaBr Brominating circulatory system was used in the synthesis of the key intermediate in a mild condition. All of the target compounds were confirmed by 1H NMR and elemental analysis and tested for their cytotoxicity against two different human cancer cell lines. The cytotoxicity assay revealed that some of the title compounds showed moderate to strong cytotoxic activities. Compound 2i was the most potent compound with the IC50 values of 9 μM against Hela cells and 15 μM against Bel–7402 cells, respectively. |
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Keywords: | Thiazole derivatives Triazole Bromination Synthesis Cytotoxicity |
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