1,2,4-Triazole D-ribose derivatives: Design, synthesis and antitumoral evaluation

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 t...

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Detalles Bibliográficos
Autores: Avanzo, Romina Edith, Anesini, Claudia Alejandra, Fascio, Mirta Liliana, Errea, María Inés, D'accorso, Norma Beatriz
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2012
País:Argentina
Institución:Consejo Nacional de Investigaciones Científicas y Técnicas
Repositorio:CONICET Digital (CONICET)
Idioma:inglés
OAI Identifier:oai:ri.conicet.gov.ar:11336/131744
Acceso en línea:http://hdl.handle.net/11336/131744
Access Level:acceso abierto
Palabra clave:1,2,4-TRIAZOLE
ANTITUMORAL ACTIVITY
D-RIBOSE
ISOXAZOLINE
https://purl.org/becyt/ford/1.4
https://purl.org/becyt/ford/1
Descripción
Sumario: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.