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  • Title: In vivo targeting of tumor-associated carbonic anhydrases using acetazolamide derivatives.
    Author: Ahlskog JK, Dumelin CE, Trüssel S, Mårlind J, Neri D.
    Journal: Bioorg Med Chem Lett; 2009 Aug 15; 19(16):4851-6. PubMed ID: 19615903.
    Abstract:
    We describe the synthesis and characterization of two acetazolamide derivatives containing either a charged fluorophore or an albumin-binding moiety, which restrict binding to carbonic anhydrase IX and XII present on tumor cells. In vivo studies showed the preferentially targeting of tumor cells by the fluorescent acetazolamide derivative and the ability of the albumin-binding acetazolamide derivative to cause tumor retardation in a SK-RC-52 xenograft model of cancer.
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