Organic & Biomolecular Chemistry · 2015 · 67 citations · 38 references
MedicineMedicinal ChemistryPharmacologyCancer PharmacologyDrug DiscoveryMolecular PharmacologyEnzyme InhibitionOncology PharmacologyStructure-activity Relationship AnalysisAnticancer ActivityCarbonic Anhydrase FunctionCarbonic Anhydrase InhibitorsCarbonic Anhydrase TargetsMedicinal Chemistry Applications
A series of 2/3/4-[(2-oxo-1,2-dihydro-3H-indol-3-ylidene)amino]benzenesulfonamides, obtained from substituted isatins and 2-, 3- or 4-aminobenzenesulfonamide, showed low nanomolar inhibitory activity against the tumor associated carbonic anhydrase (CA, EC 4.2.1.1) isoforms IX and XII - recently validated antitumor drug targets, being much less effective as inhibitors of the off-target cytosolic isoforms CA I and II.
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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
Sonia Del Prete, Daniela Vullo, Gillian M. Fisher et al. · Bioorganic & Medicinal Chemistry Letters · 2014 · 322 citations · Full text