Synthesis and anticancer activity of benzotriazole derivatives |
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| Authors: | Qiujing Li Guijun Liu Ningning Wang Huiyong Yin Zhulai Li |
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| Affiliation: | 1. Department of Pharmacy, Zhangzhou Health Vocational College, Zhangzhou, China;2. CAS Key Laboratory of Nutrition, Metabolism and Food Safety, Shanghai Institute of Nutrition and Health, Chinese Academy of Science (CAS), Shanghai, China Institute of Nutrition and Health, University of Chinese Academy of Sciences, Beijing, China;3. College of Pharmacy, Fujian Medical University, Fuzhou, China |
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| Abstract: | A series of benzotriazole (BTA) derivatives were synthesized as tyrosine protein kinase inhibitors using fragment-based design strategy. All desired compounds were synthesized with the reaction of benzotriazole, chloroacetonitrile and aromatic aldehyde using Ultrasonic-Microwave method and characterized by IR, 1H and 13C-NMR, mass spectrometry (MS) and elemental analysis. The anticancer activity of these compounds was evaluated by CCK-8 method against carcinoma VX2, lung cancer A549, stomach cancer cell lines MKN45 and MGC in vitro. The results showed that all compounds showed good antiproliferative activity. In particular, compound 2.1 showed the most prominent inhibition of VX2 cell lines with IC50 of 3.80 ± 0.75 μM. Compound 2.2 exhibited highly potent anticancer activity of stomach MGC cell lines with IC50 of 3.72 ± 0.11 μM. A549 and MKN45 cell lines were sensitive to compound 2.5 with IC50 of 5.47 ± 1.11 and 3.04 ± 0.02 μM, respectively. |
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