Synthesis and anticancer activity evaluation of a series of [1,2,4]triazolo[1,5-a]pyridinylpyridines in vitro and in vivo

•A series of [1,2,4]triazolo[1,5-a]pyridinylpyridines were synthesized.•All title compounds displayed inhibitory activity against HCT-116, U-87 MG and MCF-7 cell lines.•The SAR of target compounds was preliminarily discussed.•The compounds 1c and 2d with potent antiproliferative activities were tested for their effects on the AKT and p-AKT473.•1c exhibited potent anticancer effect in vivo.

A series of [1,2,4]triazolo[1,5-a]pyridinylpyridines were synthesized and characterized. Their antiproliferative activities in vitro were evaluated by MTT against three human cancer cell lines including HCT-116, U-87 MG and MCF-7 cell lines. The SAR of target compounds was preliminarily discussed. The compounds 1c and 2d with potent antiproliferative activities were tested for their effects on the AKT and p-AKT473. The anticancer effect of 1c was evaluated in mice bearing sarcoma S-180 model. The results suggest that the title compounds are potent anticancer agents.

Graphical abstractA series of [1,2,4]triazolo[1,5-a]pyridinylpyridines were synthesized and their anticancer effects were evaluated in vitro and in vivo.Figure optionsDownload full-size imageDownload as PowerPoint slide