Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 26, Issue 16, Pages 3892-3895Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.07.015
Keywords
Glycomimetic; Carbonic anhyrases; Sulfonamidoglycosylation
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Funding
- EU grant (Metoxia)
- UNLP (Argentina)
- CONICET (Argentina) [PIP 0701]
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A small series of N-glycosylsulfonamides incorporating the phenol moiety has been prepared by Ferrier sulfonamidoglycosylation of D-glycals. N-Glycosides were tested for the inhibition of four isoforms of carbonic anhydrase. In this study, all compounds showed good inhibitory activity against hCA I and II, with selectivity against the cytosolic hCA II versus the tumor associated isozymes. These results confirm that attaching carbohydrate moieties to CA phenol pharmacophore improves and enhances its inhibitory activity. (C) 2016 Elsevier Ltd. All rights reserved.
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