Novel sulphonamide derivatives for the treatment of cancer

The sulphonamides constitute an important class of therapeutic agents in cu rrent medicinal science. After the discovery by Gerhard Domagk, of sulphami dochrysoidine (prontosil) as the first antibiotic sulpha-drug an active met abolite of the drug, sulphanilamide, was further derivatised in order to fi nd compounds exhibiting superior antibacterial activity or different pharma cological effects. Diversification of the sulphanilamide structure led to t he serial development of improved antibiotics, insulin-releasing hypoglycae mic drugs, carbonic anhydrase- (CA) inhibitory diuretics, anti-hypertensive drugs etc. It is of particular interest that various structurally novel su lphonamide derivatives have recently been reported to show substantial anti -tumour activity in vitro and/or in vivo. Although they have a common chemi cal motif of an aromatic/heterocyclic sulphonamide, there are a variety of mechanisms for their anti-tumour action, such as disruption of microtubule assembly, cell cycle arrest in the G1 phase, functional suppression of the transcriptional activator NF-Y, angiogenesis inhibition and carbonic anhydr ase inhibition. Furthermore, some of these compounds selected via elaborate preclinical screenings are currently being evaluated in clinical trials. T his review summarises recent patents and related papers which have disclose d novel classes of sulphonamide derivatives for the treatment of cancer.