title: Amide derivatives of benzene-sulfonanilide, pharmaceutical composition thereof and method for cancer treatment using the same (US20120095092).
abstract: A series of sulfonamide derivatives incorporating an aromatic scaffold based on 1,4-phenylene diamine was prepared by a succession of five reactions. The lead molecule of these compounds was nimesulide (4-nitro-2-phenoxymethane-sulfoanilide), a cyclooxygenase (COX) inhibitor acting on both COX-1 and 2 isoforms, with some selectivity for COX-2. The new compounds from the patent are claimed to act as efficient antitumor agents, against a multitude of tumor types, such as leukemia, non-small cell lung cancer, colon cancer, brain cancer, melanoma, ovarian cancer, etc., although no COX inhibition data or other rationale to explain their biological effects are provided. As these compounds incorporate a methanesulfonamide moiety it is not unexpected that they may also appreciably inhibit tumor-associated carbonic anhydrases (CAs), such as isoforms CA IX and XII.
authors: Università degli Studi di Firenze, Dipartimento di Scienze Farmaceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino (Florence), Italy. claudiu.supuran@unifi.it
authors: Claudiu T
authors: CT
authors: Supuran
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D002257:Carbonic Anhydrase Inhibitors / Q000494:pharmacology; D016861:Cyclooxygenase Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D055808:Drug Discovery; D006801:Humans; D015394:Molecular Structure; D010330:Patents as Topic; D010655:Phenylenediamines / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000494:pharmacology*; D000096926:Benzenesulfonamides
chemical_list: D000970:Antineoplastic Agents; D002257:Carbonic Anhydrase Inhibitors; D016861:Cyclooxygenase Inhibitors; D010655:Phenylenediamines; D013449:Sulfonamides; D000096926:Benzenesulfonamides; C012655:nimesulide