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Bioorg Med Chem Lett. 2009 Aug 15;19(16):4851-6. doi: 10.1016/j.bmcl.2009.06.022. Epub 2009 Jun 13.

In vivo targeting of tumor-associated carbonic anhydrases using acetazolamide derivatives.

Author information

1
Department of Chemistry and Applied Biosciences, Institute of Pharmaceutical Sciences, ETH Zurich, CH-8093 Zurich, Switzerland.

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.

PMID:
19615903
DOI:
10.1016/j.bmcl.2009.06.022
[Indexed for MEDLINE]

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