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Synthesis and In Vitro Anticancer Activities of New 1,4-Disubstituted-1,2,3-triazoles Derivatives through Click Approach

机译:新的1,4-二取代的合成和体外抗癌活性1,2,3-三唑衍生物通过点击方法

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The synthesis of a new series 1-(3-methoxy-4-((1-phenyl-1H-1,2,3-triazole-4-yl)methoxy) phenyl)ethanone via click chemistry approach utilizing azide-alkyne cycloaddition reactions is reported in this study. The structures of all newly synthesized compounds were analyzed by IR, NMR, and Mass spectral techniques. All the newly synthesized compounds were subjected to cytotoxicity assay against a panel of three human cancer cell lines (HepG2, A549, and MCF-7) using 3-(4,5- dimethylthiazole-2-yl)-2,5-diphenyltetrazolium bromide (MTT), to check in vitro anticancer activity. Compound 5 b was found to be the most potent anticancer agents with IC_(50) value 3.42 μM, 1.26 μM, and 5.96 μM against HepG2, A549, and MCF-7 respectively. Among the tested compounds, 5a and 5q have shown notable anticancer activity as compared to the reference drug, Adriamycin.
机译:新系列1-(3-甲氧基-4 - (((((1-苯基1H-1H-1,2,3-三唑-4-基))甲氧基)苯基)苯基)乙酮通过喀哒声化学方法,利用叠氮化物环节加载反应 在这项研究中报道。 通过IR,NMR和质谱技术分析了所有新合成化合物的结构。 使用3-(4,5-二甲基硫唑-2-基)-2,5-二甲基甲基二硫代唑胺,对所有新合成化合物均对三个人类癌细胞系(HEPG2,A549和MCF-7)进行了细胞毒性测定 (MTT),检查体外抗癌活性。 发现化合物5 B分别针对HEPG2,A549和MCF-7,是IC_(50)值3.42μm,1.26μm和5.96μm的最有效的抗癌剂。 在测试化合物中,与参考药物Adrimycin相比,5A和5Q显示出显着的抗癌活性。

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