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A series of squaramates and squaramides have been synthesized and their cytotoxic activity has been investigated in different cancer cell lines.

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Abstract:In this study, the cytotoxic effects of different squaramides were tested against diverse cancer cells, such as HGC-27, HeLa, T98 and U87 cells, and non-cancer cells, such as EK293, MDCK and Vero cells. We found a disubstituted squaramide that showed an IC 50 of 1.81 μM against HGC-27 cells, which is considerably lower than the IC 50 observed in the rest of the cell lines. Furthermore, the mechanism of action of this compound was evaluated. The results indicate that the decrease in cell viability produced by the squaramide is probably caused by G 0 /G 1 cell cycle arrest and caspase-mediated apoptosis. Additionally, the cell death produced by this compound is accompanied by autophagy induction having a protective effect and no signs of cathepsin-mediated cell death or necroptosis have been observed. The creation of compounds that trigger a specific cell death subroutine is preferred since it might avoid potential side-effects and nonspecific cytotoxic effects. Therefore, this squaramide and its derivatives could be promising molecules for the treatment of gastric carcinoma.