Síntesis del glicoconjugado 1,2:5,6-di-O-isopropiliden-α-D-alofuranosil-triazol-estrona

Abstract

La síntesis y evaluación biológica de andamios moleculares derivados de triazoles unidos a fragmentos moleculares estructural y biológicamente atractivos, como son los esteroides, carbohidratos, aminoácidos etc., han demostrado su eficacia en el tratamiento de diversos tipos de cáncer, por lo cual son ampliamente utilizados para fines terapéuticos debido a su inherente actividad farmacofórica. En este trabajo se describe la síntesis de un triazol hibrido, el cual se deriva del fragmento alquino terminal, etinil-estrona y la azida orgánica 3-azida alofuranosa, mediante una reacción CuAAC usando como catalizador CuI (I).

The synthesis and biological evaluation of molecular scaffolds derived from triazoles linked to structurally and biologically attractive molecular fragments, such as steroids, carbohydrates, amino acids, etc., have demonstrated their efficacy in the treatment of various types of cancer, for which they are widely used. For these reasons this compound they are widely used for therapeutic purposes due to its inherent pharmacophoric activity., This work describes the synthesis of a hybrid triazole, which is derived from the terminal alkyne fragment, ethinyl-estrone and the organic azide 3-azide allofuranose, by means of a CuAAC reaction using CuI (I) as a catalyst.