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Bioorg Med Chem Lett. 2006 Sep 15;16(18):4846-51. Epub 2006 Jun 30.

Carbonic anhydrase inhibitors. Inhibition of the cytosolic human isozymes I and II, and the transmembrane, tumor-associated isozymes IX and XII with substituted aromatic sulfonamides activatable in hypoxic tumors.

Author information

1
Department of Chemical Technology of Drugs, Medical University of Gdansk, 80-416 Gdansk, Poland.

Abstract

Some 2-mercapto-substituted-benzenesulfonamides and their disulfides/sulfones were prepared and investigated as inhibitors of four isoforms of the zinc enzyme carbonic anhydrase (CA, EC 4.2.1.1), that is, CA I and II (cytosolic enzymes), and the tumor-associated CA IX and XII. Some mercaptans led to a consistent increase of inhibitory power (52.8- to 243-fold) over the corresponding oxidized (S-S type) derivatives, acting as potential hypoxia-activatable drugs.

PMID:
16809036
DOI:
10.1016/j.bmcl.2006.06.064
[Indexed for MEDLINE]

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