N-β-glycosyl sulfamides are selective inhibitors of the cancer associated carbonic anhydrase isoforms IX and XII.
Oscar M Rodríguez, Alfonso Maresca, Carlos A Témpera, Rodolfo D Bravo, Pedro A Colinas, Claudiu T Supuran
LADECOR, Departamento de Química, Facultad de Ciencias Exactas, Universidad Nacional de La Plata, La Plata, Argentina.
Bioorganic & medicinal chemistry letters 2011 Aug 1The 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 K(I)s in the low nanomolar range. Copyright © 2011 Elsevier Ltd. All rights reserved.
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Oscar M Rodríguez, Alfonso Maresca, Carlos A Témpera, Rodolfo D Bravo, Pedro A Colinas, Claudiu T Supuran. N-β-glycosyl sulfamides are selective inhibitors of the cancer associated carbonic anhydrase isoforms IX and XII. Bioorganic & medicinal chemistry letters. 2011 Aug 1;21(15):4447-50
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PMID: 21723123
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