These are the first results on a recently published study investigating the anticancer activity of squaramides carried out in collaboration with our collegue and friend Dr. Gemma Triola (IQAC-CISC). This article is part of a themed collection: Special issue devoted to “New Talents: Europe. Medicinal Chemistry” where Gemma was invited to contribute.
Congratulations and thank you so much for making us part of it!
“Squaramides with cytotoxic activity against human gastric carcinoma cells HGC-27: synthesis and mechanism of action” Quintana, M.; Alegre-Requena, J. V.; Marqués-López, E.; Herrera, R. P.; Triola, G. Med. Chem. Commun., 2016, Advance Article. DOI: 10.1039/C5MD00515A
Abstract. A series of squaramates and squaramides have been synthesized and their cytotoxic activity has been investigated in different cancer cell lines. Among the studied compounds, squaramide 34 showed a potent and selective cytotoxicity against the human gastric cancer cell line HGC-27. Studies directed to elucidate the mechanism of induced cell death were performed. Cell cycle distribution analysis and cell death studies showed that compound 34 induces cell cycle arrest at the G1 phase and caspase-dependent apoptosis. In conclusion, squaramide 34 can be considered a potential anticancer agent for gastric carcinoma.