A mini-library of symmetrical and unsymmetrical diglycosyl (di)sulfides, containing D-galactose, L-fucose and Nacetyl glucosamine units, were synthesized and tested for the antiproliferative activity against cervix carcinoma (HeLa) and melanoma (A375) tumor cell lines as well as healthy fibroblasts (HDF). Comparative analysis of results seems to indicate that the most relevant antiproliferative effect is not primarily influenced by interactions with galectins, as the most cytotoxic compound observed for HeLa and A375 is not a ligand for such receptors. The most active molecules against HeLa and A375 lines also exhibited a good selectivity, showing a low toxicity to HDF cells. Obtained results offer useful indications for future design of structurally simple antitumor molecules based on sugar moieties with bridging sulfur atoms
Synthesis of diglycosylated (di)sulfides and comparative evaluation of their antiproliferative effect against tumor cell lines: A focus on the nature of sugar-recognizing mediators involved / Di Gaetano, Sonia; Bedini, Emiliano; Landolfi, Alfredo; Pedone, Emilia; Pirone, Luciano; Saviano, Michele; Traboni, Serena; Capasso, Domenica; Iadonisi, Alfonso. - In: CARBOHYDRATE RESEARCH. - ISSN 0008-6215. - 482:(2019), p. 107740. [10.1016/j.carres.2019.107740]
Synthesis of diglycosylated (di)sulfides and comparative evaluation of their antiproliferative effect against tumor cell lines: A focus on the nature of sugar-recognizing mediators involved
Emiliano Bedini;Alfredo Landolfi;Serena Traboni;Domenica Capasso;Alfonso Iadonisi
2019
Abstract
A mini-library of symmetrical and unsymmetrical diglycosyl (di)sulfides, containing D-galactose, L-fucose and Nacetyl glucosamine units, were synthesized and tested for the antiproliferative activity against cervix carcinoma (HeLa) and melanoma (A375) tumor cell lines as well as healthy fibroblasts (HDF). Comparative analysis of results seems to indicate that the most relevant antiproliferative effect is not primarily influenced by interactions with galectins, as the most cytotoxic compound observed for HeLa and A375 is not a ligand for such receptors. The most active molecules against HeLa and A375 lines also exhibited a good selectivity, showing a low toxicity to HDF cells. Obtained results offer useful indications for future design of structurally simple antitumor molecules based on sugar moieties with bridging sulfur atomsI documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
