Sulfonamides incorporating boroxazolidone moieties are potent inhibitors of the transmembrane tumor-associated carbonic anhydrase isoforms IX and XII
| العنوان: | Sulfonamides incorporating boroxazolidone moieties are potent inhibitors of the transmembrane tumor-associated carbonic anhydrase isoforms IX and XII |
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| المؤلفون: | Alfonso Maresca, Andrea Scozzafava, Claudiu T. Supuran, Fatma-Zhora Smaine, Jean-Louis Montero, Marouan Rami, Jean-Yves Winum |
| المساهمون: | Institut des Biomolécules Max Mousseron [Pôle Chimie Balard] (IBMM), Ecole Nationale Supérieure de Chimie de Montpellier (ENSCM)-Institut de Chimie du CNRS (INC)-Université de Montpellier (UM)-Centre National de la Recherche Scientifique (CNRS), Laboratoire de Chimie Bioorganique, Université Badji Mokhtar - Annaba [Annaba] (UBMA), Laboratorio di Chimica Bioinorganica (LCBI), Università degli Studi di Firenze = University of Florence [Firenze] (UNIFI) |
| المصدر: | Bioorganic & Medicinal Chemistry Letters; Vol 21 Bioorganic and Medicinal Chemistry Letters Bioorganic and Medicinal Chemistry Letters, Elsevier, 2011, 21, pp.2975-2979. ⟨10.1016/j.bmcl.2011.03.055⟩ |
| سنة النشر: | 2011 |
| مصطلحات موضوعية: | Gene isoform, Boron Compounds, Stereochemistry, Boroxazolidone, Clinical Biochemistry, Pharmaceutical Science, Antineoplastic Agents, Biochemistry, Isozyme, Chemical synthesis, 03 medical and health sciences, Structure-Activity Relationship, 0302 clinical medicine, Antigens, Neoplasm, Carbonic anhydrase, Drug Discovery, medicine, Humans, Protein Isoforms, Carbonic Anhydrase IX, Carbonic Anhydrase Inhibitors, Molecular Biology, Oxazolidinones, ComputingMilieux_MISCELLANEOUS, 030304 developmental biology, Carbonic Anhydrases, chemistry.chemical_classification, 0303 health sciences, Sulfonamides, biology, Molecular Structure, [CHIM.ORGA]Chemical Sciences/Organic chemistry, Organic Chemistry, Sulfonamide (medicine), Transmembrane protein, 3. Good health, Neoplasm Proteins, Enzyme Activation, Enzyme, chemistry, 030220 oncology & carcinogenesis, biology.protein, Molecular Medicine, medicine.drug |
| الوصف: | A new series of sulfonamides was synthesized by the reaction of the boroxazolidone complex of l-lysine with isothiocyanates incorporating sulfamoyl moieties and diverse organic scaffolds. The obtained thioureas have been investigated as inhibitors of four physiologically relevant human carbonic anhydrase (hCA, EC 4.2.1.1) isoforms, hCA I, II, IX and XII. Inhibition between the low nanomolar to the micromolar range has been observed against them, with several low nanomolar and tumor-CA selective inhibitors detected. These boron-containing compounds might be useful for the management of hypoxic tumors overexpressing hCA IX/XII by means of boron neutron capture therapy, a technique not investigated so far with inhibitors of this enzyme. |
| اللغة: | English |
| تدمد: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2011.03.055 |
| DOI: | 10.1016/j.bmcl.2011.03.055⟩ |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::71a422001fc050991d369723a159df00 |
| Rights: | CLOSED |
| رقم الانضمام: | edsair.doi.dedup.....71a422001fc050991d369723a159df00 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 0960894X |
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| DOI: | 10.1016/j.bmcl.2011.03.055 |