Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 16, Pages 4851-4856Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.06.022
Keywords
Carbonic anhydrase; CA IX; CA XII; Acetazolamide; Tumor targeting
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Funding
- Swiss National Science Foundation [3100A0-105919/1]
- Swiss Cancer League (Robert-Wenner-Award)
- SWISSBRIDGE-Stammbach Foundation
- European Union [LSHC-CT-2006-037489]
- DIANA [LSHB-CT-2006037681]
- ADAMANT [HEALT-F2-2008-201342]
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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. (C) 2009 Elsevier Ltd. All rights reserved.
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