ACS Medicinal Chemistry Letters · 2015 · 12 citations · 9 references
Life SciencesMedicinal ChemistryPharmacologyBiochemical PharmacologyDrug DiscoveryEnzymologyGlycan BiosynthesisProtein GlycosylationCarbonic Anhydrase FunctionCarbonic Anhydrase InhibitorsCarbonic Anhydrase TargetsGlycal ChemistryGlycomimetic Synthesis
A general approach for the synthesis of carbonic anhydrases glycoinhibitors belonging to an aminoxysulfonamide series is presented using a Ferrier sulfonamidoglycosylation reaction on glycals. All the compounds showed good in vitro inhibitory activity against four human carbonic anhydrase isoforms, with selectivity against the cytosolic (hCA II) vs the tumor associated (hCA IX and XII) enzymes.
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Targeting carbonic anhydrase IX depletes breast cancer stem cells within the hypoxic niche
Frances E. Lock, Paul C. McDonald, Y. Lou et al. · Oncogene · 2012 · 345 citations