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ChemMedChem ; 13(14): 1395-1404, 2018 07 18.
Artículo en Inglés | MEDLINE | ID: mdl-29856519

RESUMEN

Molecules containing an (cyanovinyl)arene moiety are known as tyrphostins because of their ability to inhibit proteins from the tyrosine kinase family, an interesting target for the development of anticancer and trypanocidal drugs. In the present work, (E)-(cyanovinyl)benzeneboronic acids were synthesized by Knoevenagel condensations without the use of any catalysts in water through a simple protocol that completely avoided the use of organic solvents in the synthesis and workup process. The in vitro anticancer and trypanocidal activities of the synthesized boronic acids were also evaluated, and it was discovered that the introduction of the boronic acid functionality improved the activity of the boronic tyrphostins. In silico target fishing with the use of a chemogenomic approach suggested that tyrosine-phosphorylation-regulated kinase 1a (DYRK1A) was a potential target for some of the designed compounds.


Asunto(s)
Antineoplásicos/química , Antineoplásicos/farmacología , Compuestos de Boro/química , Compuestos de Boro/farmacología , Tripanocidas/química , Tripanocidas/farmacología , Tirfostinos/química , Tirfostinos/farmacología , Animales , Antineoplásicos/síntesis química , Compuestos de Boro/síntesis química , Línea Celular , Línea Celular Tumoral , Células Cultivadas , Enfermedad de Chagas/tratamiento farmacológico , Diseño de Fármacos , Humanos , Ratones , Modelos Moleculares , Neoplasias/tratamiento farmacológico , Proteínas Tirosina Quinasas/antagonistas & inhibidores , Tripanocidas/síntesis química , Trypanosoma cruzi/efectos de los fármacos , Tirfostinos/síntesis química
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