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合成及生物评价 3-氨基-1,2,4-三唑衍生物作为潜在的抗癌化合物。

Synthesis and biological evaluation of 3-amino-1,2,4-triazole derivatives as potential anticancer compounds.

机构信息

Université Côte d'Azur, CNRS, Institut de Chimie de Nice UMR 7272, 28 Avenue Valrose, 06108 Nice, France.

Université Côte d'Azur, CNRS UMR 7284 and INSERM U 1081, Institute for Research on Cancer and Aging (IRCAN), 28 Avenue de Valombrose, 06107 Nice, France.

出版信息

Bioorg Chem. 2020 Nov;104:104271. doi: 10.1016/j.bioorg.2020.104271. Epub 2020 Sep 8.

Abstract

Two series of compounds carrying 3-amino-1,2,4-triazole scaffold were synthesized and evaluated for their anticancer activity against a panel of cancer cell lines using XTT assay. The 1,2,4-triazole synthesis was revisited for the first series of pyridyl derivatives. The biological results revealed the efficiency of the 3-amino-1,2,4-triazole core that could not be replaced and a clear beneficial effect of a 3-bromophenylamino moiety in position 3 of the triazole for both series (compounds 2.6 and 4.6) on several cell lines tested. Moreover, our results point out an antiangiogenic activity of these compounds. Overall, the 5-aryl-3-phenylamino-1,2,4-triazole structure has promising dual anticancer activity.

摘要

两个系列的化合物携带 3-氨基-1,2,4-三唑支架被合成并评估了它们对一系列癌细胞系的抗癌活性,使用 XTT 测定法。1,2,4-三唑的合成被重新审视,为第一个系列的吡啶基衍生物。生物结果显示了 3-氨基-1,2,4-三唑核心的效率,不能被取代,并且在三唑的 3 位上的 3-溴苯氨基部分对两个系列(化合物 2.6 和 4.6)在几个测试的细胞系上都有明显的有益效果。此外,我们的结果指出了这些化合物的抗血管生成活性。总的来说,5-芳基-3-苯氨基-1,2,4-三唑结构具有有前途的双重抗癌活性。

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