Synthesis and biological evaluation of 3-amino-1,2,4-triazole derivatives as potential anticancer compounds
作者:Oleksandr Grytsai、Oksana Valiashko、Manon Penco-Campillo、Maeva Dufies、Anais Hagege、Luc Demange、Sonia Martial、Gilles Pagès、Cyril Ronco、Rachid Benhida
DOI:10.1016/j.bioorg.2020.104271
日期:2020.11
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
合成了携带3-氨基-1,2,4-三唑支架的两个系列的化合物,并使用XTT分析评估了它们对一组癌细胞系的抗癌活性。重新讨论了第一批吡啶基衍生物的1,2,4-三唑合成。生物学结果表明,对于这两个系列,不能替代的3-氨基-1,2,4-三唑核的有效性以及在三唑的3位的3-溴苯基氨基部分具有明显的有益作用(化合物2.6和4.6)在多个测试的细胞系上。此外,我们的结果指出了这些化合物的抗血管生成活性。总体而言,5-芳基-3-苯基氨基-1,2,4-三唑结构具有有前途的双重抗癌活性。