Journal
CURRENT MEDICINAL CHEMISTRY
Volume 22, Issue 24, Pages 2812-2818Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/0929867322666150716113501
Keywords
Cancer; carbonic anhydrase inhibitor; coxib; COX-2 inhibitor; oxicam
Funding
- FP7 EU project (Metoxia)
- FP7 EU project (Dynano)
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Among the class of nonsteroidal anti-inflammatory drugs (NSAIDs), COX-2 inhibitors or coxibs selectively inhibit the activity of the inducible isoform of cyclooxygenase. Moreover, there is emerging evidence that the sulfonamide-type coxibs, but not the methylsulfones, display an inhibitory activity also against several isoforms of human carbonic anhydrase (CA, EC 4.2.1.1). In this regard, celecoxib and valdecoxib, possessing a primary sulfonamide that binds to the zinc ion at the active site of the enzyme, are nanomolar inhibitors of the cancer-related hCA IX isoform. Also meloxicam and lornoxicam, NSAIDs belonging to the class of oxicams, that contain a cyclic tertiary sulfonamide moiety, inhibit this isoform at low micromolar concentrations. The multiple pharmacological effects of the sulfonamide anti-inflammatory agents could be ascribed to the dual inhibition of CA and COX enzymes, supporting the evidence that inflammation and hypoxia pathways are involved in cancer onset and progression and suggesting that the antitumoral activity of these compounds should be further explored for their possible use in the polypharmacology of cancer prevention and therapy.
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