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Synthesis and anticancer activity of benzotriazole derivatives
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2019-12-25 , DOI: 10.1002/jhet.3859 Qiujing Li 1 , Guijun Liu 2, 3 , Ningning Wang 2, 3 , Huiyong Yin 2, 3 , Zhulai Li 4
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2019-12-25 , DOI: 10.1002/jhet.3859 Qiujing Li 1 , Guijun Liu 2, 3 , Ningning Wang 2, 3 , Huiyong Yin 2, 3 , Zhulai Li 4
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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.
中文翻译：
苯并三唑衍生物的合成及其抗癌活性
使用基于片段的设计策略，合成了一系列苯并三唑（BTA）衍生物作为酪氨酸蛋白激酶抑制剂。使用超声波-微波法，通过苯并三唑，氯乙腈和芳族醛的反应合成所有所需化合物，并通过IR，1 H和13 C-NMR，质谱（MS）和元素分析进行表征。通过CCK-8方法评估了这些化合物在体外对VX2癌，肺癌A549癌，胃癌细胞系MKN45和MGC的抗癌活性。结果表明，所有化合物均显示出良好的抗增殖活性。尤其是，化合物2.1对IC 50表现出最显着的VX2细胞抑制作用为3.80±0.75μM。化合物2.2对胃MGC细胞系表现出高度有效的抗癌活性，IC 50为3.72±0.11μM。A549和MKN45细胞系对化合物2.5敏感，IC 50分别为5.47±1.11和3.04±0.02μM。
更新日期：2019-12-27
中文翻译：
苯并三唑衍生物的合成及其抗癌活性
使用基于片段的设计策略，合成了一系列苯并三唑（BTA）衍生物作为酪氨酸蛋白激酶抑制剂。使用超声波-微波法，通过苯并三唑，氯乙腈和芳族醛的反应合成所有所需化合物，并通过IR，1 H和13 C-NMR，质谱（MS）和元素分析进行表征。通过CCK-8方法评估了这些化合物在体外对VX2癌，肺癌A549癌，胃癌细胞系MKN45和MGC的抗癌活性。结果表明，所有化合物均显示出良好的抗增殖活性。尤其是，化合物2.1对IC 50表现出最显着的VX2细胞抑制作用为3.80±0.75μM。化合物2.2对胃MGC细胞系表现出高度有效的抗癌活性，IC 50为3.72±0.11μM。A549和MKN45细胞系对化合物2.5敏感，IC 50分别为5.47±1.11和3.04±0.02μM。
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