Artículo

N-β-Glycosyl sulfamides are selective inhibitors of the cancer associated carbonic anhydrase isoforms IX and XII

Rodríguez, Oscar Mariano; Maresca, Alfonso; Témpera, Carlos AgustínIcon ; Bravo, Rodolfo Daniel; Colinas, Pedro AlfonsoIcon ; Supuran, Claudiu T.
Fecha de publicación: 08/2011
Editorial: Pergamon-Elsevier Science Ltd
Revista: Biorganic and Medicinal Chemistry Letters
ISSN: 0960-894X
Idioma: Inglés
Tipo de recurso: Artículo publicado
Clasificación temática:

Resumen

The transmembrane isoforms of carbonic anhydrase (CA IX and XII) have been shown to be linked to carcinogenesis and their inhibition to arrest primary tumor and metastases growth. In this Letter, we present a series of peracetylated and deprotected N-β-glycosyl sulfamides that were tested for the inhibition of 4 carbonic anhydrase isoforms: the cytosolic hCA I and hCA II and transmembrane tumor-associated IX and XII. Compounds 1–4 and 6–8 selectively target cancer-associated CAs (IX and XII) with KIs in the low nanomolar range.
Palabras clave: Glycosyl sulfamides , Carbonic anhydrase , Targeted therapies , Cancer
 
Archivos asociados
Thumbnail
 
Tamaño: 302.6Kb
Formato: PDF
.
Licencia
info:eu-repo/semantics/openAccess Excepto donde se diga explícitamente, este item se publica bajo la siguiente descripción: Creative Commons Attribution-NonCommercial-ShareAlike 2.5 Unported (CC BY-NC-SA 2.5)
Identificadores
URI: http://hdl.handle.net/11336/95100
URL: https://www.sciencedirect.com/science/article/pii/S0960894X11008146
DOI: http://dx.doi.org/10.1016/j.bmcl.2011.06.031
Colecciones
Articulos(CCT - LA PLATA)
Articulos de CTRO.CIENTIFICO TECNOL.CONICET - LA PLATA
Citación
Rodríguez, Oscar Mariano; Maresca, Alfonso; Témpera, Carlos Agustín; Bravo, Rodolfo Daniel; Colinas, Pedro Alfonso; et al.; N-β-Glycosyl sulfamides are selective inhibitors of the cancer associated carbonic anhydrase isoforms IX and XII; Pergamon-Elsevier Science Ltd; Biorganic and Medicinal Chemistry Letters; 21; 15; 8-2011; 4447-4450
Compartir
Altmétricas