N-beta-glycosyl sulfamides are selective inhibitors of the cancer associated carbonic anhydrase isoforms IX and XII.

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Rodriguez OM, Maresca A, Tempera CA, Bravo RD, Colinas PA, Supuran CT

N-beta-glycosyl sulfamides are selective inhibitors of the cancer associated carbonic anhydrase isoforms IX and XII.

Bioorg Med Chem Lett. 2011 Aug 1;21(15):4447-50. doi: 10.1016/j.bmcl.2011.06.031. Epub 2011 Jun 16.

PubMed ID

21723123 [ View in PubMed

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Abstract

The transmembrane isoforms of carbonic anhydrase (CA IX and XII) have been shown to be linked to carcinogenesis and their inhibition to arrest primary tumor and metastases growth. In this Letter, we present a series of peracetylated and deprotected N-beta-glycosyl sulfamides that were tested for the inhibition of 4 carbonic anhydrase isoforms: the cytosolic hCA I and hCA II and transmembrane tumor-associated IX and XII. Compounds 1-4 and 6-8 selectively target cancer-associated CAs (IX and XII) with K(I)s in the low nanomolar range.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Topiramate	Carbonic anhydrase 1	Ki (nM)	250	N/A	N/A	Details
Topiramate	Carbonic anhydrase 2	Ki (nM)	5	N/A	N/A	Details