4.5 Review

Novel sulphonamide derivatives for the treatment of cancer

Journal

EXPERT OPINION ON THERAPEUTIC PATENTS
Volume 10, Issue 11, Pages 1725-1740

Publisher

TAYLOR & FRANCIS LTD
DOI: 10.1517/13543776.10.11.1725

Keywords

angiogenesis; antimitotic; anti-tumour; carbonic anhydrase; cell cycle; G1 phase; M phase; NF-Y; sulphonamide; sulphonylurea; tubulin; xenograft

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The sulphonamides constitute an important class of therapeutic agents in current medicinal science. After the discovery by Gerhard Domagk, of sulphamidochrysoidine (prontosil) as the first antibiotic sulpha-drug an active metabolite of the drug, sulphanilamide, was further derivatised in order to find compounds exhibiting superior antibacterial activity or different pharmacological effects. Diversification of the sulphanilamide structure led to the serial development of improved antibiotics, insulin-releasing hypoglycaemic drugs, carbonic anhydrase- (CA) inhibitory diuretics, anti-hypertensive drugs etc. It is of particular interest that various structurally novel sulphonamide derivatives have recently been reported to show substantial anti-tumour activity in vitro and/or in vivo. Although they have a common chemical 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 anhydrase inhibition. Furthermore, some of these compounds selected via elaborate preclinical screenings are currently being evaluated in clinical trials. This review summarises recent patents and related papers which have disclosed novel classes of sulphonamide derivatives for the treatment of cancer.

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