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.

Amide derivatives of benzene-sulfonanilide, pharmaceutical composition thereof and method for cancer treatment using the same (US20120095092) / C. T. Supuran. - In: EXPERT OPINION ON THERAPEUTIC PATENTS. - ISSN 1354-3776. - STAMPA. - 22:(2012), pp. 1251-1255. [10.1517/13543776.2012.712687]

Amide derivatives of benzene-sulfonanilide, pharmaceutical composition thereof and method for cancer treatment using the same (US20120095092).

SUPURAN, CLAUDIU TRANDAFIR
2012

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.
2012
22
1251
1255
C. T. Supuran
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Utilizza questo identificatore per citare o creare un link a questa risorsa: https://hdl.handle.net/2158/776419
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