Development of potent carbonic anhydrase inhibitors incorporating both sulfonamide and sulfamide groups (440 views)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2012; 55(15): 6776-6783.
Export to BibTeX Export to EndNote
Paper type: Journal Article,
Impact factor: 5.614, 5-year impact factor: 5.383
Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-84864917818&partnerID=40&md5=91e508eac5d24d0676acb14a19b8fd1c
Keywords: 4 (4 Acetamidophenylsulfonamido)benzoic Acid, 4 (4 Aminophenylsulfonamido)benzoic Acid, 4 [4 (sulfamoylamino)phenylsulfonamido] N (4 Sulfamoylphenethyl)benzamide, Acetazolamide, Carbonate Dehydratase Ii, Carbonate Dehydratase Inhibitor, Diclofenamide, Ethoxzolamide, N Sulfamoyl 4 Aminobenzene Sulfonamide, Sulfanilamide, Unclassified Drug, Zinc Ion, Article, Controlled Study, Drug Potency, Drug Protein Binding, Drug Structure, Enzyme Active Site, Structure Analysis, X Ray Crystallography, Carbonic Anhydrase Inhibitors, X-Ray, Enzyme Assays, Humans, Isoenzymes, Models, Molecular, Protein Conformation, Structure-Activity Relationship, 4 (4 Acetamidophenylsulfonamido) Benzoic Acid, 4 (4 Aminophenylsulfonamido) Benzoic Acid, 4 [4 (sulfamoylamino) Phenylsulfonamido] N (4 Sulfamoylphenethyl) Benzamide,
Affiliations:
*** IBB - CNR ***
Istituto di Biostrutture e Bioimmagini-CNR, via Mezzocannone 16, 80134 Napoli, Italy
Institut des Biomolécules Max Mousseron (IBMM), UMR 5247, CNRS-UM1-UM2, 8 rue de l'Ecole Normale, 34296 Montpellier Cedex, France
Universitaè Degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze), Italy
Universita Degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze), Italy
References:
Alterio, V., Di Fiore, A., D'Ambrosio, K., Supuran, C.T., De Simone, G., Multiple Binding Modes of Inhibitors to Carbonic Anhydrases: How to Design Specific Drugs Targeting 15 Different Isoforms? (2012) Chem. Rev., 112. , DOI: 10.1021/cr200176
Supuran, C.T., Carbonic anhydrases: Novel therapeutic applications for inhibitors and activators (2008) Nat. Rev. Drug Discovery, 7, pp. 168-181
MacK, E.T., Snyder, P.W., Perez-Castillejos, R., Bilgicer, B., Moustakas, D.T., Butte, M.J., Whitesides, G.M., Dependence of Avidity on Linker Length for a Bivalent Ligand-Bivalent Receptor Model System (2012) J. Am. Chem. Soc., 134, pp. 333-345
Winum, J.Y., Vullo, D., Casini, A., Montero, J.L., Scozzafava, A., Supuran, C.T., Carbonic anhydrase inhibitors. Inhibition of cytosolic isozymes i and II and transmembrane, tumor-associated isozyme IX with sulfamates including EMATE also acting as steroid sulfatase inhibitors (2003) J. Med. Chem., 46, pp. 2197-2204
Abbate, F., Winum, J.Y., Potter, B.V., Casini, A., Montero, J.L., Scozzafava, A., Supuran, C.T., Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with EMATE, a dual inhibitor of carbonic anhydrases and steroid sulfatase (2004) Bioorg. Med. Chem. Lett., 14, pp. 231-234
Winum, J.Y., Scozzafava, A., Montero, J.L., Supuran, C.T., Design of zinc binding functions for carbonic anhydrase inhibitors (2008) Curr. Pharm. Des., 14, pp. 615-621
Supuran, C.T., Diuretics: From classical carbonic anhydrase inhibitors to novel applications of the sulfonamides (2008) Curr. Pharm. Des., 14, pp. 641-648
Mincione, F., Scozzafava, A., Supuran, C.T., (2009) Drug Design of Zinc-Enzyme Inhibitors: Functional, Structural, and Disease Applications, pp. 139-154. , Supuran, C. T. Winum, J. Y. Wiley: Hoboken
Thiry, A., Dogneè, J.M., Masereel, B., Supuran, C.T., Carbonic Anhydrase Inhibitors as Anticonvulsant Agents (2007) Curr. Top. Med. Chem., 7, pp. 855-864
De Simone, G., Di Fiore, A., Supuran, C.T., Are carbonic anhydrase inhibitors suitable for obtaining antiobesity drugs? (2008) Curr. Pharm. Des., 14, pp. 655-660
Dubois, L., Lieuwes, N.G., Maresca, A., Thiry, A., Supuran, C.T., Scozzafava, A., Wouters, B.G., Lambin, P., Imaging of CA IX with fluorescent labelled sulfonamides distinguishes hypoxic and (re)-oxygenated cells in a xenograft tumour model (2009) Radiother. Oncol., 92, pp. 423-428
Ahlskog, J.K., Dumelin, C.E., Trüssel, S., Marlind, J., Neri, D., In vivo targeting of tumor-associated carbonic anhydrases using acetazolamide derivatives (2009) Bioorg. Med. Chem. Lett., 19, pp. 4851-4856
Buller, F., Steiner, M., Frey, K., Mircsof, D., Scheuermann, J., Kalisch, M., Bühlmann, P., Neri, D., Selection of Carbonic Anhydrase IX Inhibitors from One Million DNA-Encoded Compounds (2011) ACS Chem. Biol., 6, pp. 336-344
Zatovicova, M., Jelenska, L., Hulikova, A., Csaderova, L., Ditte, Z., Ditte, P., Goliasova, T., Pastorekova, S., Carbonic anhydrase IX as an anticancer therapy target: Preclinical evaluation of internalizing monoclonal antibody directed to catalytic domain (2010) Curr. Pharm. Des., 16, pp. 3255-3263
Neri, D., Supuran, C.T., Interfering with pH regulation in tumours as a therapeutic strategy (2011) Nat. Rev. Drug Discovery, 10, pp. 767-777
Abbate, F., Supuran, C.T., Scozzafava, A., Orioli, P., Stubbs, M.T., Klebe, G., Nonaromatic sulfonamide group as an ideal anchor for potent human carbonic anhydrase inhibitors: Role of hydrogen-bonding networks in ligand binding and drug design (2002) J. Med. Chem., 45, pp. 3583-3587
De Simone, G., Supuran, C.T., Antiobesity carbonic anhydrase inhibitors (2007) Curr. Top. Med. Chem., 7, pp. 879-884
Supuran, C.T., Di Fiore, A., De Simone, G., Carbonic anhydrase inhibitors as emerging drugs for the treatment of obesity (2008) Expert Opin. Emerging Drugs, 13, pp. 383-392
Thiry, A., Dogné, J.M., Supuran, C.T., Masereel, B., Anticonvulsant sulfonamides/sulfamates/sulfamides with carbonic anhydrase inhibitory activity: Drug design and mechanism of action (2008) Curr. Pharm. Des., 14, pp. 661-671
Cecchi, A., Winum, J.Y., Innocenti, A., Vullo, D., Montero, J.L., Scozzafava, A., Supuran, C.T., Carbonic anhydrase inhibitors: Synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides derived from 4-isothiocyanato-benzolamide (2004) Bioorg. Med. Chem. Lett., 14, pp. 5775-5780
Puccetti, L., Fasolis, G., Cecchi, A., Winum, J.Y., Gamberi, A., Montero, J.L., Scozzafava, A., Supuran, C.T., Carbonic anhydrase inhibitors: Synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating thioureido-sulfanilyl scaffolds (2005) Bioorg. Med. Chem. Lett., 15, pp. 2359-2364
Casini, A., Winum, J.Y., Montero, J.L., Scozzafava, A., Supuran, C.T., Carbonic anhydrase inhibitors: Inhibition of cytosolic isozymes i and II with sulfamide derivatives (2003) Bioorg. Med. Chem. Lett., 13, pp. 837-840
Supuran, C.T., Clare, B.W., Carbonic anhydrase inhibitors. Part 24. A quantitative structure-activity study of positively-charged sulfonamide inhibitors (1995) Eur. J. Med. Chem., 30, pp. 687-696
Eriksson, A.E., Jones, T.A., Liljas, A., Refined structure of human carbonic anhydrase II at 2.0 Å resolution (1988) Proteins, 4, pp. 274-282
Khalifah, R.G., The carbon dioxide hydration activity of carbonic anhydrase. I. Stop-flow kinetic studies on the native human isoenzymes B and C (1971) J. Biol. Chem., 246, pp. 2561-2573
Pocker, Y., Stone, J.T., The catalytic versatility of erythrocyte carbonic anhydrase. III. Kinetic studies of the enzyme-catalyzed hydrolysis of p-nitrophenyl acetate (1967) Biochemistry, 6, pp. 668-678
Innocenti, A., Supuran, C.T., Paraoxon, 4-nitrophenyl phosphate and acetate are substrates of α- But not of β-, γ- And ζ-carbonic anhydrases (2010) Bioorg. Med. Chem. Lett., 20, pp. 6208-6212
Pastor-Navarro, N., García-Bover, C., Maquieira, A., Puchades, R., Specific polyclonal-based immunoassays for sulfathiazole (2004) Anal. Bioanal. Chem., 379, pp. 1088-1099
Okada, M., Iwashita, S., Koizumi, N., Efficient general method for sulfamoylation of a hydroxyl group (2000) Tetrahedron Lett., 41, pp. 7047-7051
Appel, R., Berger, G., Hydrazodiaulfamides (1958) Chem. Ber., 91, pp. 1339-1341
Otwinowski, Z., Minor, W., Processing of X-ray Diffraction Data Collected in Oscillation Mode (1997) Methods Enzymol., 276, pp. 307-326
Brunger, A.T., Adams, P.D., Clore, G.M., De Lano, W.L., Gros, P., Grosse-Kunstleve, R.W., Jiang, J.S., Warren, G.L., Crystallography & NMR system: A new software suite for macromolecular structure determination (1998) Acta Crystallogr., Sect. D, 54, pp. 905-921
Jones, T.A., Zou, J.Y., Cowan, S.W., Kjeldgaard, M., Improved methods for building protein models in electron density maps and the location of errors in these models (1991) Acta Crystallogr., Sect. A, 47, pp. 110-119
Laskowski, R.A., MacArthur, M.W., Moss, D.S., Thornton, J.M., PROCHECK: A program to check the stereochemical quality of protein structures (1993) J. Appl. Crystallogr., 26, pp. 283-291
Supuran, C. T., Carbonic anhydrases: Novel therapeutic applications for inhibitors and activators (2008) Nat. Rev. Drug Discovery, 7, pp. 168-181
MacK, E. T., Snyder, P. W., Perez-Castillejos, R., Bilgicer, B., Moustakas, D. T., Butte, M. J., Whitesides, G. M., Dependence of Avidity on Linker Length for a Bivalent Ligand-Bivalent Receptor Model System (2012) J. Am. Chem. Soc., 134, pp. 333-345
Winum, J. Y., Vullo, D., Casini, A., Montero, J. L., Scozzafava, A., Supuran, C. T., Carbonic anhydrase inhibitors. Inhibition of cytosolic isozymes i and II and transmembrane, tumor-associated isozyme IX with sulfamates including EMATE also acting as steroid sulfatase inhibitors (2003) J. Med. Chem., 46, pp. 2197-2204
Winum, J. Y., Scozzafava, A., Montero, J. L., Supuran, C. T., Design of zinc binding functions for carbonic anhydrase inhibitors (2008) Curr. Pharm. Des., 14, pp. 615-621
Supuran, C. T., Diuretics: From classical carbonic anhydrase inhibitors to novel applications of the sulfonamides (2008) Curr. Pharm. Des., 14, pp. 641-648
Thiry, A., Dogne, J. M., Masereel, B., Supuran, C. T., Carbonic Anhydrase Inhibitors as Anticonvulsant Agents (2007) Curr. Top. Med. Chem., 7, pp. 855-864
Ahlskog, J. K., Dumelin, C. E., Tr ssel, S., Marlind, J., Neri, D., In vivo targeting of tumor-associated carbonic anhydrases using acetazolamide derivatives (2009) Bioorg. Med. Chem. Lett., 19, pp. 4851-4856
Supuran, C. T., Di Fiore, A., De Simone, G., Carbonic anhydrase inhibitors as emerging drugs for the treatment of obesity (2008) Expert Opin. Emerging Drugs, 13, pp. 383-392
Thiry, A., Dogn, J. M., Supuran, C. T., Masereel, B., Anticonvulsant sulfonamides/sulfamates/sulfamides with carbonic anhydrase inhibitory activity: Drug design and mechanism of action (2008) Curr. Pharm. Des., 14, pp. 661-671
Supuran, C. T., Clare, B. W., Carbonic anhydrase inhibitors. Part 24. A quantitative structure-activity study of positively-charged sulfonamide inhibitors (1995) Eur. J. Med. Chem., 30, pp. 687-696
Eriksson, A. E., Jones, T. A., Liljas, A., Refined structure of human carbonic anhydrase II at 2. 0 resolution (1988) Proteins, 4, pp. 274-282
Khalifah, R. G., The carbon dioxide hydration activity of carbonic anhydrase. I. Stop-flow kinetic studies on the native human isoenzymes B and C (1971) J. Biol. Chem., 246, pp. 2561-2573
Brunger, A. T., Adams, P. D., Clore, G. M., De Lano, W. L., Gros, P., Grosse-Kunstleve, R. W., Jiang, J. S., Warren, G. L., Crystallography & NMR system: A new software suite for macromolecular structure determination (1998) Acta Crystallogr., Sect. D, 54, pp. 905-921
Jones, T. A., Zou, J. Y., Cowan, S. W., Kjeldgaard, M., Improved methods for building protein models in electron density maps and the location of errors in these models (1991) Acta Crystallogr., Sect. A, 47, pp. 110-119
Laskowski, R. A., MacArthur, M. W., Moss, D. S., Thornton, J. M., PROCHECK: A program to check the stereochemical quality of protein structures (1993) J. Appl. Crystallogr., 26, pp. 283-291
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2012; 55(15): 6776-6783.
Export to BibTeX Export to EndNote
Paper type: Journal Article,
Impact factor: 5.614, 5-year impact factor: 5.383
Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-84864917818&partnerID=40&md5=91e508eac5d24d0676acb14a19b8fd1c
Keywords: 4 (4 Acetamidophenylsulfonamido)benzoic Acid, 4 (4 Aminophenylsulfonamido)benzoic Acid, 4 [4 (sulfamoylamino)phenylsulfonamido] N (4 Sulfamoylphenethyl)benzamide, Acetazolamide, Carbonate Dehydratase Ii, Carbonate Dehydratase Inhibitor, Diclofenamide, Ethoxzolamide, N Sulfamoyl 4 Aminobenzene Sulfonamide, Sulfanilamide, Unclassified Drug, Zinc Ion, Article, Controlled Study, Drug Potency, Drug Protein Binding, Drug Structure, Enzyme Active Site, Structure Analysis, X Ray Crystallography, Carbonic Anhydrase Inhibitors, X-Ray, Enzyme Assays, Humans, Isoenzymes, Models, Molecular, Protein Conformation, Structure-Activity Relationship, 4 (4 Acetamidophenylsulfonamido) Benzoic Acid, 4 (4 Aminophenylsulfonamido) Benzoic Acid, 4 [4 (sulfamoylamino) Phenylsulfonamido] N (4 Sulfamoylphenethyl) Benzamide,
Affiliations:
*** IBB - CNR ***
Istituto di Biostrutture e Bioimmagini-CNR, via Mezzocannone 16, 80134 Napoli, Italy
Institut des Biomolécules Max Mousseron (IBMM), UMR 5247, CNRS-UM1-UM2, 8 rue de l'Ecole Normale, 34296 Montpellier Cedex, France
Universitaè Degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze), Italy
Universita Degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze), Italy
References:
Alterio, V., Di Fiore, A., D'Ambrosio, K., Supuran, C.T., De Simone, G., Multiple Binding Modes of Inhibitors to Carbonic Anhydrases: How to Design Specific Drugs Targeting 15 Different Isoforms? (2012) Chem. Rev., 112. , DOI: 10.1021/cr200176
Supuran, C.T., Carbonic anhydrases: Novel therapeutic applications for inhibitors and activators (2008) Nat. Rev. Drug Discovery, 7, pp. 168-181
MacK, E.T., Snyder, P.W., Perez-Castillejos, R., Bilgicer, B., Moustakas, D.T., Butte, M.J., Whitesides, G.M., Dependence of Avidity on Linker Length for a Bivalent Ligand-Bivalent Receptor Model System (2012) J. Am. Chem. Soc., 134, pp. 333-345
Winum, J.Y., Vullo, D., Casini, A., Montero, J.L., Scozzafava, A., Supuran, C.T., Carbonic anhydrase inhibitors. Inhibition of cytosolic isozymes i and II and transmembrane, tumor-associated isozyme IX with sulfamates including EMATE also acting as steroid sulfatase inhibitors (2003) J. Med. Chem., 46, pp. 2197-2204
Abbate, F., Winum, J.Y., Potter, B.V., Casini, A., Montero, J.L., Scozzafava, A., Supuran, C.T., Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with EMATE, a dual inhibitor of carbonic anhydrases and steroid sulfatase (2004) Bioorg. Med. Chem. Lett., 14, pp. 231-234
Winum, J.Y., Scozzafava, A., Montero, J.L., Supuran, C.T., Design of zinc binding functions for carbonic anhydrase inhibitors (2008) Curr. Pharm. Des., 14, pp. 615-621
Supuran, C.T., Diuretics: From classical carbonic anhydrase inhibitors to novel applications of the sulfonamides (2008) Curr. Pharm. Des., 14, pp. 641-648
Mincione, F., Scozzafava, A., Supuran, C.T., (2009) Drug Design of Zinc-Enzyme Inhibitors: Functional, Structural, and Disease Applications, pp. 139-154. , Supuran, C. T. Winum, J. Y. Wiley: Hoboken
Thiry, A., Dogneè, J.M., Masereel, B., Supuran, C.T., Carbonic Anhydrase Inhibitors as Anticonvulsant Agents (2007) Curr. Top. Med. Chem., 7, pp. 855-864
De Simone, G., Di Fiore, A., Supuran, C.T., Are carbonic anhydrase inhibitors suitable for obtaining antiobesity drugs? (2008) Curr. Pharm. Des., 14, pp. 655-660
Dubois, L., Lieuwes, N.G., Maresca, A., Thiry, A., Supuran, C.T., Scozzafava, A., Wouters, B.G., Lambin, P., Imaging of CA IX with fluorescent labelled sulfonamides distinguishes hypoxic and (re)-oxygenated cells in a xenograft tumour model (2009) Radiother. Oncol., 92, pp. 423-428
Ahlskog, J.K., Dumelin, C.E., Trüssel, S., Marlind, J., Neri, D., In vivo targeting of tumor-associated carbonic anhydrases using acetazolamide derivatives (2009) Bioorg. Med. Chem. Lett., 19, pp. 4851-4856
Buller, F., Steiner, M., Frey, K., Mircsof, D., Scheuermann, J., Kalisch, M., Bühlmann, P., Neri, D., Selection of Carbonic Anhydrase IX Inhibitors from One Million DNA-Encoded Compounds (2011) ACS Chem. Biol., 6, pp. 336-344
Zatovicova, M., Jelenska, L., Hulikova, A., Csaderova, L., Ditte, Z., Ditte, P., Goliasova, T., Pastorekova, S., Carbonic anhydrase IX as an anticancer therapy target: Preclinical evaluation of internalizing monoclonal antibody directed to catalytic domain (2010) Curr. Pharm. Des., 16, pp. 3255-3263
Neri, D., Supuran, C.T., Interfering with pH regulation in tumours as a therapeutic strategy (2011) Nat. Rev. Drug Discovery, 10, pp. 767-777
Abbate, F., Supuran, C.T., Scozzafava, A., Orioli, P., Stubbs, M.T., Klebe, G., Nonaromatic sulfonamide group as an ideal anchor for potent human carbonic anhydrase inhibitors: Role of hydrogen-bonding networks in ligand binding and drug design (2002) J. Med. Chem., 45, pp. 3583-3587
De Simone, G., Supuran, C.T., Antiobesity carbonic anhydrase inhibitors (2007) Curr. Top. Med. Chem., 7, pp. 879-884
Supuran, C.T., Di Fiore, A., De Simone, G., Carbonic anhydrase inhibitors as emerging drugs for the treatment of obesity (2008) Expert Opin. Emerging Drugs, 13, pp. 383-392
Thiry, A., Dogné, J.M., Supuran, C.T., Masereel, B., Anticonvulsant sulfonamides/sulfamates/sulfamides with carbonic anhydrase inhibitory activity: Drug design and mechanism of action (2008) Curr. Pharm. Des., 14, pp. 661-671
Cecchi, A., Winum, J.Y., Innocenti, A., Vullo, D., Montero, J.L., Scozzafava, A., Supuran, C.T., Carbonic anhydrase inhibitors: Synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides derived from 4-isothiocyanato-benzolamide (2004) Bioorg. Med. Chem. Lett., 14, pp. 5775-5780
Puccetti, L., Fasolis, G., Cecchi, A., Winum, J.Y., Gamberi, A., Montero, J.L., Scozzafava, A., Supuran, C.T., Carbonic anhydrase inhibitors: Synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating thioureido-sulfanilyl scaffolds (2005) Bioorg. Med. Chem. Lett., 15, pp. 2359-2364
Casini, A., Winum, J.Y., Montero, J.L., Scozzafava, A., Supuran, C.T., Carbonic anhydrase inhibitors: Inhibition of cytosolic isozymes i and II with sulfamide derivatives (2003) Bioorg. Med. Chem. Lett., 13, pp. 837-840
Supuran, C.T., Clare, B.W., Carbonic anhydrase inhibitors. Part 24. A quantitative structure-activity study of positively-charged sulfonamide inhibitors (1995) Eur. J. Med. Chem., 30, pp. 687-696
Eriksson, A.E., Jones, T.A., Liljas, A., Refined structure of human carbonic anhydrase II at 2.0 Å resolution (1988) Proteins, 4, pp. 274-282
Khalifah, R.G., The carbon dioxide hydration activity of carbonic anhydrase. I. Stop-flow kinetic studies on the native human isoenzymes B and C (1971) J. Biol. Chem., 246, pp. 2561-2573
Pocker, Y., Stone, J.T., The catalytic versatility of erythrocyte carbonic anhydrase. III. Kinetic studies of the enzyme-catalyzed hydrolysis of p-nitrophenyl acetate (1967) Biochemistry, 6, pp. 668-678
Innocenti, A., Supuran, C.T., Paraoxon, 4-nitrophenyl phosphate and acetate are substrates of α- But not of β-, γ- And ζ-carbonic anhydrases (2010) Bioorg. Med. Chem. Lett., 20, pp. 6208-6212
Pastor-Navarro, N., García-Bover, C., Maquieira, A., Puchades, R., Specific polyclonal-based immunoassays for sulfathiazole (2004) Anal. Bioanal. Chem., 379, pp. 1088-1099
Okada, M., Iwashita, S., Koizumi, N., Efficient general method for sulfamoylation of a hydroxyl group (2000) Tetrahedron Lett., 41, pp. 7047-7051
Appel, R., Berger, G., Hydrazodiaulfamides (1958) Chem. Ber., 91, pp. 1339-1341
Otwinowski, Z., Minor, W., Processing of X-ray Diffraction Data Collected in Oscillation Mode (1997) Methods Enzymol., 276, pp. 307-326
Brunger, A.T., Adams, P.D., Clore, G.M., De Lano, W.L., Gros, P., Grosse-Kunstleve, R.W., Jiang, J.S., Warren, G.L., Crystallography & NMR system: A new software suite for macromolecular structure determination (1998) Acta Crystallogr., Sect. D, 54, pp. 905-921
Jones, T.A., Zou, J.Y., Cowan, S.W., Kjeldgaard, M., Improved methods for building protein models in electron density maps and the location of errors in these models (1991) Acta Crystallogr., Sect. A, 47, pp. 110-119
Laskowski, R.A., MacArthur, M.W., Moss, D.S., Thornton, J.M., PROCHECK: A program to check the stereochemical quality of protein structures (1993) J. Appl. Crystallogr., 26, pp. 283-291
Supuran, C. T., Carbonic anhydrases: Novel therapeutic applications for inhibitors and activators (2008) Nat. Rev. Drug Discovery, 7, pp. 168-181
MacK, E. T., Snyder, P. W., Perez-Castillejos, R., Bilgicer, B., Moustakas, D. T., Butte, M. J., Whitesides, G. M., Dependence of Avidity on Linker Length for a Bivalent Ligand-Bivalent Receptor Model System (2012) J. Am. Chem. Soc., 134, pp. 333-345
Winum, J. Y., Vullo, D., Casini, A., Montero, J. L., Scozzafava, A., Supuran, C. T., Carbonic anhydrase inhibitors. Inhibition of cytosolic isozymes i and II and transmembrane, tumor-associated isozyme IX with sulfamates including EMATE also acting as steroid sulfatase inhibitors (2003) J. Med. Chem., 46, pp. 2197-2204
Winum, J. Y., Scozzafava, A., Montero, J. L., Supuran, C. T., Design of zinc binding functions for carbonic anhydrase inhibitors (2008) Curr. Pharm. Des., 14, pp. 615-621
Supuran, C. T., Diuretics: From classical carbonic anhydrase inhibitors to novel applications of the sulfonamides (2008) Curr. Pharm. Des., 14, pp. 641-648
Thiry, A., Dogne, J. M., Masereel, B., Supuran, C. T., Carbonic Anhydrase Inhibitors as Anticonvulsant Agents (2007) Curr. Top. Med. Chem., 7, pp. 855-864
Ahlskog, J. K., Dumelin, C. E., Tr ssel, S., Marlind, J., Neri, D., In vivo targeting of tumor-associated carbonic anhydrases using acetazolamide derivatives (2009) Bioorg. Med. Chem. Lett., 19, pp. 4851-4856
Supuran, C. T., Di Fiore, A., De Simone, G., Carbonic anhydrase inhibitors as emerging drugs for the treatment of obesity (2008) Expert Opin. Emerging Drugs, 13, pp. 383-392
Thiry, A., Dogn, J. M., Supuran, C. T., Masereel, B., Anticonvulsant sulfonamides/sulfamates/sulfamides with carbonic anhydrase inhibitory activity: Drug design and mechanism of action (2008) Curr. Pharm. Des., 14, pp. 661-671
Supuran, C. T., Clare, B. W., Carbonic anhydrase inhibitors. Part 24. A quantitative structure-activity study of positively-charged sulfonamide inhibitors (1995) Eur. J. Med. Chem., 30, pp. 687-696
Eriksson, A. E., Jones, T. A., Liljas, A., Refined structure of human carbonic anhydrase II at 2. 0 resolution (1988) Proteins, 4, pp. 274-282
Khalifah, R. G., The carbon dioxide hydration activity of carbonic anhydrase. I. Stop-flow kinetic studies on the native human isoenzymes B and C (1971) J. Biol. Chem., 246, pp. 2561-2573
Brunger, A. T., Adams, P. D., Clore, G. M., De Lano, W. L., Gros, P., Grosse-Kunstleve, R. W., Jiang, J. S., Warren, G. L., Crystallography & NMR system: A new software suite for macromolecular structure determination (1998) Acta Crystallogr., Sect. D, 54, pp. 905-921
Jones, T. A., Zou, J. Y., Cowan, S. W., Kjeldgaard, M., Improved methods for building protein models in electron density maps and the location of errors in these models (1991) Acta Crystallogr., Sect. A, 47, pp. 110-119
Laskowski, R. A., MacArthur, M. W., Moss, D. S., Thornton, J. M., PROCHECK: A program to check the stereochemical quality of protein structures (1993) J. Appl. Crystallogr., 26, pp. 283-291
Development of potent carbonic anhydrase inhibitors incorporating both sulfonamide and sulfamide groups
A series of compounds incorporating both sulfonamide and sulfamide as zinc-binding groups (ZBGs) are reported as inhibitors of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1). Crystallographic studies on the complex of hCA II with the lead compound of this series, namely, 4-sulfamido- benzenesulfonamide, revealed the binding of two molecules in the enzyme active site cavity, the first one canonically coordinated to the zinc ion by means of the sulfonamide group and the second one located at the entrance of the cavity. This observation led to the design of elongated molecules incorporating these two ZBGs, separated by a linker of proper length, to allow the simultaneous binding to these different sites. The long inhibitors indeed showed around 10 times better enzyme inhibitory properties as compared to the shorter molecules against four physiologically relevant human (h) isoforms, hCA I, II, IX, and XII. © 2012 American Chemical Society.
A series of compounds incorporating both sulfonamide and sulfamide as zinc-binding groups (ZBGs) are reported as inhibitors of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1). Crystallographic studies on the complex of hCA II with the lead compound of this series, namely, 4-sulfamido- benzenesulfonamide, revealed the binding of two molecules in the enzyme active site cavity, the first one canonically coordinated to the zinc ion by means of the sulfonamide group and the second one located at the entrance of the cavity. This observation led to the design of elongated molecules incorporating these two ZBGs, separated by a linker of proper length, to allow the simultaneous binding to these different sites. The long inhibitors indeed showed around 10 times better enzyme inhibitory properties as compared to the shorter molecules against four physiologically relevant human (h) isoforms, hCA I, II, IX, and XII. © 2012 American Chemical Society.
Development of potent carbonic anhydrase inhibitors incorporating both sulfonamide and sulfamide groups
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Development of potent carbonic anhydrase inhibitors incorporating both sulfonamide and sulfamide groups
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Alterio V, Langella E, Buonanno M, Esposito D, Nocentini A, Berrino E, Bua S, Polentarutti M, Supuran CT, Monti SM, De Simone G
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Impact Factor: 7.271
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De Simone G, Bua S, Supuran CT, Alterio V
* Benzyl alcohol inhibits carbonic anhydrases by anchoring to the zinc coordinated water molecule (8 views)
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Impact Factor: 3.575
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Mishra CB, Kumari S, Angeli A, Monti SM, Buonanno M, Tiwari M, Supuran CT
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Impact Factor: 6.253
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Altug C, Gunes H, Nocentini A, Monti SM, Buonanno M, Supuran CT
* Synthesis of isoxazole-containing sulfonamides with potent carbonic anhydrase II and VII inhibitory properties (277 views)
Bioorg Med Chem (ISSN: 0968-0896, 1464-3391, 0968-0896linking), 2017 Feb 15; 25(4): 1456-1464.
Impact Factor: 2.881
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Angapelly S, Ramya PVS, Angeli A, Monti SM, Buonanno M, Alvala M, Supuran CT, Arifuddin M
* Discovery of 4-sulfamoyl-phenyl-β-lactams as a new class of potent carbonic anhydrase isoforms I, II, IV and VII inhibitors: The first example of subnanomolar CA IV inhibitors (241 views)
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Impact Factor: 2.881
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D'Ambrosio K, Carradori S, Monti SM, Buonanno M, Secci D, Vullo D, Supuran CT, De Simone G
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Impact Factor: 6.567
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Iqbal J, Al-rashida M, Durdagi S, Alterio V, Di Fiore A
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Impact Factor: 2.134
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Di Fiore A, Alterio V, Monti SM, De Simone G, D’Ambrosio K
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Int J Mol Sc (ISSN: 1422-0067, 1661-6596, 1422-0067linking), 2015; 16(7): 15456-15480.
Impact Factor: 3.257
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De Simone G, Alterio V, Supuran CT
* Exploiting the hydrophobic and hydrophilic binding sites for designing carbonic anhydrase inhibitors (439 views)
Expert Opin Drug Discov (ISSN: 1746-0441), 2013 Jul; 8(7): 793-810.
Impact Factor: 3.467
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Truppo E, Supuran CT, Sandomenico A, Vullo D, Innocenti A, Di Fiore A, Alterio V, De Simone G, Monti SM
* Carbonic anhydrase VII is S-glutathionylated without loss of catalytic activity and affinity for sulfonamide inhibitors (350 views)
Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2012 Feb 15; 22(4): 1560-1564.
Impact Factor: 2.338
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Viparelli F, Monti SM, De Simone G, Innocenti A, Scozzafava A, Xu Y, Morel FMM, Supuran CT
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Impact Factor: 2.661
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Di Fiore A, Truppo E, Supuran CT, Alterio V, Dathan N, Bootorabi F, Parkkila S, Monti SM, De Simone G
* Crystal structure of the C183S/C217S mutant of human CA VII in complex with acetazolamide (315 views)
Bioorg Med Chem Lett (ISSN: 0960-894x), 2010 Sep 1; 20(17): 5023-5026.
Impact Factor: 2.661
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Guler OO, De Simone G, Supuran CT
* Drug design studies of the novel antitumor targets carbonic anhydrase IX and XII (523 views)
Curr Med Chem (ISSN: 0929-8673, 1875-533x, 1875-533xelectronic), 2010; 17(15): 1516-1526.
Impact Factor: 4.63
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Kapucu OL, Nobili F, Varrone A, Booij J, Vander Borght T, Nagren K, Darcourt J, Tatsch K, Van Laere KJ
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Impact Factor: 4.531
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Alterio V, Hilvo M, Di Fiore A, Supuran CT, Pan P, Parkkila S, Scaloni A, Pastorek J, Pastorekova S, Pedone C, Scozzafava A, Monti SM, De Simone G
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Impact Factor: 9.432
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De Simone G, Scozzafava A, Supuran CT
* Which Carbonic Anhydrases are Targeted by the Antiepileptic Sulfonamides and Sulfamates? (333 views)
Chem Biol Drug Des (ISSN: 1747-0277, 1747-0285), 2009 Sep; 74(3): 317-321.
Impact Factor: 2.473
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Di Fiore A, Monti SM, Hilvo M, Parkkila S, Romano V, Scaloni A, Pedone C, Scozzafava A, Supuran CT, De Simone G
* Crystal structure of human carbonic anhydrase XIII and its complex with the inhibitor acetazolamide (442 views)
Proteins (ISSN: 1097-0134, 0887-3585, 1097-0134electronic), 2009 Jan; 74(1): 164-175.
Impact Factor: 3.085
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Hilvo M, Baranauskiene L, Salzano AM, Scaloni A, Matulis D, Innocenti A, Scozzafava A, Monti SM, Di Fiore A, De Simone G, Lindfors M, Janis J, Valjakka J, Pastorekova S, Pastorek J, Kulomaa MS, Nordlund HR, Supuran CT, Parkkila S
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Jbc Papers (ISSN: 0021-9258, 1083-351x, 0021-9258linking), 2008 Oct 10; 283(41): 27799-27809.
Impact Factor: 5.52
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Supuran CT, Di Fiore A, De Simone G
* Carbonic anhydrase inhibitors as emerging drugs for the treatment of obesity (505 views)
Expert Opin Emerg Drugsexpert Opinion On Emerging Drugs (ISSN: 1472-8214), 2008 Jun; 13(2): 383-392.
Impact Factor: 3.08
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Innocenti A, Scozzafava A, Parkkila S, Puccetti L, De Simone G, Supuran CT
* Investigations of the esterase, phosphatase, and sulfatase activities of the cytosolic mammalian carbonic anhydrase isoforms I, II, and XIII with 4-nitrophenyl esters as substrates (350 views)
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Impact Factor: 2.531
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Leese MP, Jourdan FL, Gaukroger K, Mahon MF, Newman SP, Foster PA, Stengel C, Regis-Lydi S, Ferrandis E, Di Fiore A, De Simone G, Supuran CT, Purohit A, Reed MJ, Potter BVL
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Impact Factor: 4.898
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De Simone G, Di Fiore A, Supuran CT
* Are carbonic anhydrase inhibitors suitable for obtaining antiobesity drugs? (448 views)
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Impact Factor: 4.399
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D'Ambrosio K, Masereel B, Thiry A, Scozzafava A, Supuran CT, De Simone G
* Carbonic anhydrase inhibitors: Binding of indanesulfonamides to the human isoform II (348 views)
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Impact Factor: 3.15
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Hilvo M, Innocenti A, Monti SM, De Simone G, Supuran CT, Parkkila S
* Recent advances in research on the most novel carbonic anhydrases, CA XIII and XV (431 views)
Curr Pharm Des Current Pharmaceutical Design (ISSN: 1381-6128, 1873-4286), 2008; 14(7): 672-678.
Impact Factor: 4.399
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Calabrese V, Mancuso C, Calvani M, Rizzarelli E, Butterfield DA, Stella AM
* Nitric oxide in the central nervous system: neuroprotection versus neurotoxicity (628 views)
Nature Reviews Neuroscience (ISSN: 1471-0048), 2007 Oct; 8(10): 766-775.
Impact Factor: 24.52
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Vitale RM, Pedone C, Amodeo P, Antel J, Wurl M, Scozzafava A, Supuran CT, De Simone G
* Molecular modeling study for the binding of zonisamide and topiramate to the human mitochondrial carbonic anhydrase isoform VA (323 views)
Bioorg Med Chem (ISSN: 0968-0896, 1464-3391, 1464-3391electronic), 2007 Jun 15; 15(12): 4152-4158.
Impact Factor: 2.662
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De Simone G, Supuran CT
* Antiobesity carbonic anhydrase inhibitors (422 views)
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Impact Factor: 4.325
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Leese MP, Leblond B, Smith A, Newman SP, Di Fiore A, De Simone G, Supuran CT, Purohit A, Reed MJ, Potter BVL
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De Simone G, Vitale RM, Di Fiore A, Pedone C, Scozzafava A, Montero JL, Winum JY, Supuran CT
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Impact Factor: 5.115
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Di Fiore A, Pedone C, D'Ambrosio K, Scozzafava A, De Simone G, Supuran CT
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Menchise V, De Simone G, Alterio V, Di Fiore A, Pedone C, Scozzafava A, Supuran CT
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Impact Factor: 4.926
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De Simone G, Di Fiore A, Menchise V, Pedone C, Antel J, Casini A, Scozzafava A, Wurl M, Supuran CT
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Impact Factor: 2.478
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Di Fiore A, De Simone G, Menchise V, Pedone C, Casini A, Scozzafava A, Supuran CT
* Carbonic anhydrase inhibitors: X-ray crystal structure of a benzenesulfonamide strong CA II and CA IX inhibitor bearing a pentafluorophenylaminothioureido tail in complex with isozyme II (478 views)
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Impact Factor: 2.478
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Soricelli A, Postiglione A, Cuocolo A, De Chiara S, Ruocco A, Brunetti A, Salvatore M, Ell PJ
EFFECT OF ADENOSINE ON CEREBRAL BLOOD-FLOW AS EVALUATED BY SINGLE-PHOTON EMISSION COMPUTED-TOMOGRAPHY IN NORMAL SUBJECTS AND IN PATIENTS WITH OCCLUSIVE CAROTID DISEASE - A COMPARISON WITH ACETAZOLAMIDE (249 views)
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Mancini M, De Chiara S, Ferrara LA, Gallotta G, Postiglione A
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15th World Congress Angiology Rome, 1989; 20(4): 284-284.
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* Zeta-carbonic anhydrases show CS(2) hydrolase activity: A new metabolic carbon acquisition pathway in diatoms? (23 views)
Comput Struct Biotechnol J (ISSN: 2001-0370linking), 2021 Jun 5; 19: 3427-3436.
Impact Factor: 7.271
View Export to BibTeX Export to EndNote
De Simone G, Bua S, Supuran CT, Alterio V
* Benzyl alcohol inhibits carbonic anhydrases by anchoring to the zinc coordinated water molecule (8 views)
Biochem Biophys Res Commun (ISSN: 0006-291xlinking), 2021 Apr 9; 548: 217-221.
Impact Factor: 3.575
View Export to BibTeX Export to EndNote
Mishra CB, Kumari S, Angeli A, Monti SM, Buonanno M, Tiwari M, Supuran CT
* Discovery of Benzenesulfonamides with Potent Human Carbonic Anhydrase Inhibitory and Effective Anticonvulsant Action: Design, Synthesis, and Pharmacological Assessment (737 views)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2017 Mar 23; 60(6): 2456-2469.
Impact Factor: 6.253
View Export to BibTeX Export to EndNote
Altug C, Gunes H, Nocentini A, Monti SM, Buonanno M, Supuran CT
* Synthesis of isoxazole-containing sulfonamides with potent carbonic anhydrase II and VII inhibitory properties (277 views)
Bioorg Med Chem (ISSN: 0968-0896, 1464-3391, 0968-0896linking), 2017 Feb 15; 25(4): 1456-1464.
Impact Factor: 2.881
View Export to BibTeX Export to EndNote
Angapelly S, Ramya PVS, Angeli A, Monti SM, Buonanno M, Alvala M, Supuran CT, Arifuddin M
* Discovery of 4-sulfamoyl-phenyl-β-lactams as a new class of potent carbonic anhydrase isoforms I, II, IV and VII inhibitors: The first example of subnanomolar CA IV inhibitors (241 views)
Bioorg Med Chem (ISSN: 0968-0896, 1464-3391, 0968-0896linking), 2017; 25(2): 539-544.
Impact Factor: 2.881
View Export to BibTeX Export to EndNote
D'Ambrosio K, Carradori S, Monti SM, Buonanno M, Secci D, Vullo D, Supuran CT, De Simone G
* Out of the active site binding pocket for carbonic anhydrase inhibitors (360 views) (PDF 234 views)
Chem Commun (ISSN: 1359-7345, 1364-548x, 1364-548xelectronic), 2015 Jan 7; 51(2): 302-305.
Impact Factor: 6.567
View Export to BibTeX Export to EndNote
Iqbal J, Al-rashida M, Durdagi S, Alterio V, Di Fiore A
* Recent developments of carbonic anhydrase inhibitors as potential drugs (392 views)
Biomed Res Int (ISSN: 2314-6133, 2314-6141), 2015; 2015: 174178-174178.
Impact Factor: 2.134
View Export to BibTeX Export to EndNote
Di Fiore A, Alterio V, Monti SM, De Simone G, D’Ambrosio K
* Thermostable carbonic anhydrases in biotechnological applications (453 views)
Int J Mol Sc (ISSN: 1422-0067, 1661-6596, 1422-0067linking), 2015; 16(7): 15456-15480.
Impact Factor: 3.257
View Export to BibTeX Export to EndNote
De Simone G, Alterio V, Supuran CT
* Exploiting the hydrophobic and hydrophilic binding sites for designing carbonic anhydrase inhibitors (439 views)
Expert Opin Drug Discov (ISSN: 1746-0441), 2013 Jul; 8(7): 793-810.
Impact Factor: 3.467
View Export to BibTeX Export to EndNote
Truppo E, Supuran CT, Sandomenico A, Vullo D, Innocenti A, Di Fiore A, Alterio V, De Simone G, Monti SM
* Carbonic anhydrase VII is S-glutathionylated without loss of catalytic activity and affinity for sulfonamide inhibitors (350 views)
Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2012 Feb 15; 22(4): 1560-1564.
Impact Factor: 2.338
View Export to BibTeX Export to EndNote
Viparelli F, Monti SM, De Simone G, Innocenti A, Scozzafava A, Xu Y, Morel FMM, Supuran CT
* Inhibition Of The R1 Fragment Of The Cadmium-Containing Zeta-Class Carbonic Anhydrase From The Diatom Thalassiosira Weissflogii With Anions (318 views)
Bioorganic & Medicinal Chemistry Letters (ISSN: 0960-894x), 2010 Sep 15; 20(16): 4745-4748.
Impact Factor: 2.661
View Export to BibTeX Export to EndNote
Di Fiore A, Truppo E, Supuran CT, Alterio V, Dathan N, Bootorabi F, Parkkila S, Monti SM, De Simone G
* Crystal structure of the C183S/C217S mutant of human CA VII in complex with acetazolamide (315 views)
Bioorg Med Chem Lett (ISSN: 0960-894x), 2010 Sep 1; 20(17): 5023-5026.
Impact Factor: 2.661
View Export to BibTeX Export to EndNote
Guler OO, De Simone G, Supuran CT
* Drug design studies of the novel antitumor targets carbonic anhydrase IX and XII (523 views)
Curr Med Chem (ISSN: 0929-8673, 1875-533x, 1875-533xelectronic), 2010; 17(15): 1516-1526.
Impact Factor: 4.63
View Export to BibTeX Export to EndNote
Kapucu OL, Nobili F, Varrone A, Booij J, Vander Borght T, Nagren K, Darcourt J, Tatsch K, Van Laere KJ
* EANM procedure guideline for brain perfusion SPECT using Tc-99m-labelled radiopharmaceuticals, version (525 views)
Eur J Nucl Med (ISSN: 1619-7070, 1619-7089, 0340-6997), 2009 Dec; 36(12): 2093-2102.
Impact Factor: 4.531
View Export to BibTeX Export to EndNote
Alterio V, Hilvo M, Di Fiore A, Supuran CT, Pan P, Parkkila S, Scaloni A, Pastorek J, Pastorekova S, Pedone C, Scozzafava A, Monti SM, De Simone G
* Crystal structure of the catalytic domain of the tumor-associated human carbonic anhydrase IX (523 views)
P Natl Acad Sci Usa (ISSN: 0027-8424, 1091-6490, 0027-8424print), 2009 Sep 22; 106(38): 16233-16238.
Impact Factor: 9.432
View Export to BibTeX Export to EndNote
De Simone G, Scozzafava A, Supuran CT
* Which Carbonic Anhydrases are Targeted by the Antiepileptic Sulfonamides and Sulfamates? (333 views)
Chem Biol Drug Des (ISSN: 1747-0277, 1747-0285), 2009 Sep; 74(3): 317-321.
Impact Factor: 2.473
View Export to BibTeX Export to EndNote
Di Fiore A, Monti SM, Hilvo M, Parkkila S, Romano V, Scaloni A, Pedone C, Scozzafava A, Supuran CT, De Simone G
* Crystal structure of human carbonic anhydrase XIII and its complex with the inhibitor acetazolamide (442 views)
Proteins (ISSN: 1097-0134, 0887-3585, 1097-0134electronic), 2009 Jan; 74(1): 164-175.
Impact Factor: 3.085
View Export to BibTeX Export to EndNote
Hilvo M, Baranauskiene L, Salzano AM, Scaloni A, Matulis D, Innocenti A, Scozzafava A, Monti SM, Di Fiore A, De Simone G, Lindfors M, Janis J, Valjakka J, Pastorekova S, Pastorek J, Kulomaa MS, Nordlund HR, Supuran CT, Parkkila S
* Biochemical characterization of CA IX, one of the most active carbonic anhydrase isozymes (421 views)
Jbc Papers (ISSN: 0021-9258, 1083-351x, 0021-9258linking), 2008 Oct 10; 283(41): 27799-27809.
Impact Factor: 5.52
View Export to BibTeX Export to EndNote
Supuran CT, Di Fiore A, De Simone G
* Carbonic anhydrase inhibitors as emerging drugs for the treatment of obesity (505 views)
Expert Opin Emerg Drugsexpert Opinion On Emerging Drugs (ISSN: 1472-8214), 2008 Jun; 13(2): 383-392.
Impact Factor: 3.08
View Export to BibTeX Export to EndNote
Innocenti A, Scozzafava A, Parkkila S, Puccetti L, De Simone G, Supuran CT
* Investigations of the esterase, phosphatase, and sulfatase activities of the cytosolic mammalian carbonic anhydrase isoforms I, II, and XIII with 4-nitrophenyl esters as substrates (350 views)
Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2008 Apr 1; 18(7): 2267-2271.
Impact Factor: 2.531
View Export to BibTeX Export to EndNote
Leese MP, Jourdan FL, Gaukroger K, Mahon MF, Newman SP, Foster PA, Stengel C, Regis-Lydi S, Ferrandis E, Di Fiore A, De Simone G, Supuran CT, Purohit A, Reed MJ, Potter BVL
* Structure-activity relationships of C-17 cyano-substituted estratrienes as anticancer agents (429 views)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2008 Mar 13; 51(5): 1295-1308.
Impact Factor: 4.898
View Export to BibTeX Export to EndNote
De Simone G, Di Fiore A, Supuran CT
* Are carbonic anhydrase inhibitors suitable for obtaining antiobesity drugs? (448 views)
Curr Pharm Des Current Pharmaceutical Design (ISSN: 1381-6128, 1873-4286), 2008 Mar; 14(7): 655-660.
Impact Factor: 4.399
View Export to BibTeX Export to EndNote
D'Ambrosio K, Masereel B, Thiry A, Scozzafava A, Supuran CT, De Simone G
* Carbonic anhydrase inhibitors: Binding of indanesulfonamides to the human isoform II (348 views)
Chemmedchem (ISSN: 1860-7179, 1860-7187, 1860-7187electronic), 2008 Mar; 3(3): 473-477.
Impact Factor: 3.15
View Export to BibTeX Export to EndNote
Hilvo M, Innocenti A, Monti SM, De Simone G, Supuran CT, Parkkila S
* Recent advances in research on the most novel carbonic anhydrases, CA XIII and XV (431 views)
Curr Pharm Des Current Pharmaceutical Design (ISSN: 1381-6128, 1873-4286), 2008; 14(7): 672-678.
Impact Factor: 4.399
View Export to BibTeX Export to EndNote
Calabrese V, Mancuso C, Calvani M, Rizzarelli E, Butterfield DA, Stella AM
* Nitric oxide in the central nervous system: neuroprotection versus neurotoxicity (628 views)
Nature Reviews Neuroscience (ISSN: 1471-0048), 2007 Oct; 8(10): 766-775.
Impact Factor: 24.52
View Export to BibTeX Export to EndNote
Vitale RM, Pedone C, Amodeo P, Antel J, Wurl M, Scozzafava A, Supuran CT, De Simone G
* Molecular modeling study for the binding of zonisamide and topiramate to the human mitochondrial carbonic anhydrase isoform VA (323 views)
Bioorg Med Chem (ISSN: 0968-0896, 1464-3391, 1464-3391electronic), 2007 Jun 15; 15(12): 4152-4158.
Impact Factor: 2.662
View Export to BibTeX Export to EndNote
De Simone G, Supuran CT
* Antiobesity carbonic anhydrase inhibitors (422 views)
Curr Top Med Chem (ISSN: 1568-0266, 1568-0266linking, 1873-4294electronic), 2007; 7(9): 879-884.
Impact Factor: 4.325
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Leese MP, Leblond B, Smith A, Newman SP, Di Fiore A, De Simone G, Supuran CT, Purohit A, Reed MJ, Potter BVL
* 2-substituted estradiol bis-sulfamates, multitargeted antitumor agents: synthesis, in vitro SAR, protein crystallography, and in vivo activity (909 views)
J Med Chem (ISSN: 0022-2623print, 0022-2623linking, 1520-4804), 2006 Dec 28; 49(26): 7683-7696.
Impact Factor: 5.115
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De Simone G, Vitale RM, Di Fiore A, Pedone C, Scozzafava A, Montero JL, Winum JY, Supuran CT
* Carbonic anhydrase inhibitors: Hypoxia-activatable sulfonamides incorporating disulfide bonds that target the tumor-associated isoform IX (459 views)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2006 Sep 7; 49(18): 5544-5551.
Impact Factor: 5.115
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Di Fiore A, Pedone C, D'Ambrosio K, Scozzafava A, De Simone G, Supuran CT
* Carbonic anhydrase inhibitors: Valdecoxib binds to a different active site region of the human isoform II as compared to the structurally related cyclooxygenase II 'selective' inhibitor celecoxib (301 views)
Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2006 Jan 15; 16(2): 437-442.
Impact Factor: 2.538
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Menchise V, De Simone G, Alterio V, Di Fiore A, Pedone C, Scozzafava A, Supuran CT
* Carbonic anhydrase inhibitors: Stacking with Phe131 determines active site binding region of inhibitors as exemplified by the X-ray crystal structure of a membrane-impermeant antitumor sulfonamide complexed with isozyme II (466 views)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2005 Sep 8; 48(18): 5721-5727.
Impact Factor: 4.926
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De Simone G, Di Fiore A, Menchise V, Pedone C, Antel J, Casini A, Scozzafava A, Wurl M, Supuran CT
* Carbonic anhydrase inhibitors. Zonisamide is an effective inhibitor of the cytosolic isozyme II and mitochondrial isozyme V: solution and X-ray crystallographic studies (386 views)
Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2005 May 2; 15(9): 2315-2320.
Impact Factor: 2.478
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Di Fiore A, De Simone G, Menchise V, Pedone C, Casini A, Scozzafava A, Supuran CT
* Carbonic anhydrase inhibitors: X-ray crystal structure of a benzenesulfonamide strong CA II and CA IX inhibitor bearing a pentafluorophenylaminothioureido tail in complex with isozyme II (478 views)
Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2005 Apr 1; 15(7): 1937-1942.
Impact Factor: 2.478
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Soricelli A, Postiglione A, Cuocolo A, De Chiara S, Ruocco A, Brunetti A, Salvatore M, Ell PJ
EFFECT OF ADENOSINE ON CEREBRAL BLOOD-FLOW AS EVALUATED BY SINGLE-PHOTON EMISSION COMPUTED-TOMOGRAPHY IN NORMAL SUBJECTS AND IN PATIENTS WITH OCCLUSIVE CAROTID DISEASE - A COMPARISON WITH ACETAZOLAMIDE (249 views)
Stroke (ISSN: 0039-2499), 1995 Sep; 26(9): 1572-1576.
Impact Factor: 4.323
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Mancini M, De Chiara S, Ferrara LA, Gallotta G, Postiglione A
TRANSCRANIAL DOPPLER EVALUATION OF CEREBROVASCULAR REACTIVITY TO ACETAZOLAMIDE IN NORMAL SUBJECTS (635 views)
15th World Congress Angiology Rome, 1989; 20(4): 284-284.
Impact Factor: 0
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35 Records (33 excluding Abstracts).
Total impact factor: 156.554 (151.439 excluding Abstracts).
Total 5 year impact factor: 152.426 (146.922 excluding Abstracts).
Total impact factor: 156.554 (151.439 excluding Abstracts).
Total 5 year impact factor: 152.426 (146.922 excluding Abstracts).
440 views. Last view on Wednesday 05 October 2022, 0:52:22
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