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      Fluoroenesulphonamides: N-sulphonylurea isosteres showing nanomolar selective cancer-related transmembrane human carbonic anhydrase inhibition

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          Abstract

          After hydrofluorination of ynesulphonamides in superacid or in the presence of hydrofluoric acid/base reagents, a series of α-fluoroenamides has been synthesised and tested for the inhibition of carbonic anhydrase (CA, EC 4.2.1.1) isoforms. This study reveals a new, highly selective family of cancer-related transmembrane human (h) CA IX/XII inhibitors. These original fluorinated ureido isosters do not inhibit the widespread cytosolic isoforms hCA I and II and selectively inhibit the transmembrane cancer-related hCA IX and XII, offering interesting new leads for future studies.

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          Most cited references 34

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          Interfering with pH regulation in tumours as a therapeutic strategy.

          The high metabolic rate of tumours often leads to acidosis and hypoxia in poorly perfused regions. Tumour cells have thus evolved the ability to function in a more acidic environment than normal cells. Key pH regulators in tumour cells include: isoforms 2, 9 and 12 of carbonic anhydrase, isoforms of anion exchangers, Na+/HCO3- co-transporters, Na+/H+ exchangers, monocarboxylate transporters and the vacuolar ATPase. Both small molecules and antibodies targeting these pH regulators are currently at various stages of clinical development. These antitumour mechanisms are not exploited by the classical cancer drugs and therefore represent a new anticancer drug discovery strategy.
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            The carbon dioxide hydration activity of carbonic anhydrase. I. Stop-flow kinetic studies on the native human isoenzymes B and C.

             R Khalifah (1971)
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              Multiple binding modes of inhibitors to carbonic anhydrases: how to design specific drugs targeting 15 different isoforms?

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                Author and article information

                Journal
                J Enzyme Inhib Med Chem
                J Enzyme Inhib Med Chem
                IENZ
                ienz20
                Journal of Enzyme Inhibition and Medicinal Chemistry
                Taylor & Francis
                1475-6366
                1475-6374
                2018
                30 April 2018
                : 33
                : 1
                : 804-808
                Affiliations
                [a ]IC2MP-UMR CNRS 7582, Superacid Group–Organic Synthesis Team, Université de Poitiers , Poitiers, France;
                [b ]Department NEUROFARBA–Pharmaceutical and Nutraceutical Chemistry Section, Università degli Studi di Firenze , Sesto Fiorentino, Florence, Italy;
                [c ]Institut Lavoisier de Versailles, UMR CNRS 8180, Universitée de Versailles Saint-Quentin-en-Yvelines , Versailles, France;
                [d ]Laboratoire de Chimie Organique, Service de Chimie et Physico Chimie Organiques, Université Libre de Bruxelles , Brussels, Belgium
                Author notes
                CONTACT Claudiu T. Supuran claudiu.supuran@ 123456unifi.it Department NEUROFARBA–Pharmaceutical and Nutraceutical Chemistry Section, Università degli Studi di Firenze , Sesto Fiorentino, Florence, Italy;
                Sebastien Thibaudeau sebastien.thibaudeau@ 123456univ-poitiers.fr IC2MP-UMR CNRS 7582, Superacid Group–Organic Synthesis Team, Université de Poitiers , Poitiers, France
                Article
                1461097
                10.1080/14756366.2018.1461097
                6009971
                29706097
                © 2018 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group.

                This is an Open Access article distributed under the terms of the Creative Commons Attribution License ( http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

                Page count
                Pages: 5, Words: 4162
                Product
                Categories
                Short Communication

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