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