info:eu-repo/semantics/article
1,2,4-Triazole D-ribose derivatives: Design, synthesis and antitumoral evaluation
Fecha
2012-01Registro en:
Avanzo, Romina Edith; Anesini, Claudia Alejandra; Fascio, Mirta Liliana; Errea, María Inés; D'accorso, Norma Beatriz; 1,2,4-Triazole D-ribose derivatives: Design, synthesis and antitumoral evaluation; Elsevier France-editions Scientifiques Medicales Elsevier; European Journal of Medical Chemistry; 47; 1; 1-2012; 104-110
0223-5234
CONICET Digital
CONICET
Autor
Avanzo, Romina Edith
Anesini, Claudia Alejandra
Fascio, Mirta Liliana
Errea, María Inés
D'accorso, Norma Beatriz
Resumen
Herein we report the design, synthesis and characterization of novel 1,2,4-triazole D-ribose derivatives, as well as their synthetic precursors.The antitumoral activity against T cell lymphoma cell line of these products was studied. Structures containing a 1,2,4-triazolic ring linked by sulfur to the carbohydrate moiety showed a moderate antiproliferative activity. The presence of the second heterocyclic ring did not show significant changes in their biological activity. Meanwhile, structures with 3-thiobenzyl-5-substituted-1,2,4-triazole ring linked by nitrogen leads to compounds with a biphasic behavior, stimulating cell proliferation at low concentrations and inhibiting it at higher ones. An increment in the polarity was associated with a decrease in the activity of the evaluated compounds.A preliminary antitumoral screening pointed the 1,2,4-triazolic structures linked to protected sugars as promising leaders for further studies.