Development of potent carbonic anhydrase inhibitors incorporating both sulfonamide and sulfamide groups (410 views visite)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2012; 55(15): 6776-6783.
Export to Esporta in BibTeX Export to Esporta in EndNote
Paper type Tipo di articolo: Journal Article,
Impact factor: 5.614, 5-year impact factor Impact factor a 5 anni: 5.383
Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-84864917818&partnerID=40&md5=91e508eac5d24d0676acb14a19b8fd1c
Keywords Parole chiave: 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 Affiliazioni:
*** 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
Institut des Biomol cules Max Mousseron (IBMM), UMR 5247, CNRS-UM1-UM2, 8 rue de l'Ecole Normale, 34296 Montpellier Cedex, France
Universita Degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze), Italy
References Riferimenti:
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 Esporta in BibTeX Export to Esporta in EndNote
Paper type Tipo di articolo: Journal Article,
Impact factor: 5.614, 5-year impact factor Impact factor a 5 anni: 5.383
Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-84864917818&partnerID=40&md5=91e508eac5d24d0676acb14a19b8fd1c
Keywords Parole chiave: 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 Affiliazioni:
*** 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
Institut des Biomol cules Max Mousseron (IBMM), UMR 5247, CNRS-UM1-UM2, 8 rue de l'Ecole Normale, 34296 Montpellier Cedex, France
Universita Degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze), Italy
References Riferimenti:
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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* Probing Molecular Interactions between Human Carbonic Anhydrases (hCAs) and a Novel Class of Benzenesulfonamides (354 visite)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2017 May 25; 60(10): 4316-4326.
Impact Factor: 6.253
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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 (336 visite)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2017 Mar 23; 60(6): 2456-2469.
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 (257 visite)
Bioorg Med Chem (ISSN: 0968-0896, 1464-3391), 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 (221 visite)
Bioorg Med Chem (ISSN: 0968-0896, 1464-3391), 2017; 25(2): 539-544.
Impact Factor: 2.881
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Monti SM, Supuran CT, De Simone G
* DPP-4 inhibitors: a patent review (2012 - 2014) (341 visite)
Expert Opin Ther Pat (ISSN: 1354-3776, 1744-7674electronic), 2015 Feb; 25(2): 209-236.
Impact Factor: 4.626
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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 (345 visite) (PDF 229 visite)
Chem Commun (ISSN: 1359-7345, 1364-548x, 1364-548xelectronic), 2015 Jan 7; 51(2): 302-305.
Impact Factor: 6.567
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Ceruso M, Carta F, Osman SM, Alothman Z, Monti SM, Supuran CT
* Inhibition studies of bacterial, fungal and protozoan β-class carbonic anhydrases with Schiff bases incorporating sulfonamide moieties (330 visite)
Bioorg Med Chem (ISSN: 0968-0896, 1464-3391), 2015; 23(15): 4181-4187.
Impact Factor: 2.923
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Iqbal J, Al-rashida M, Durdagi S, Alterio V, Di Fiore A
* Recent developments of carbonic anhydrase inhibitors as potential drugs (381 visite)
Biomed Res Int (ISSN: 2314-6133, 2314-6141), 2015; 2015: 174178-174178.
Impact Factor: 2.134
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Di Fiore A, Alterio V, Monti SM, De Simone G, D’Ambrosio K
* Thermostable carbonic anhydrases in biotechnological applications (412 visite)
Int J Mol Sc (ISSN: 1422-0067, 1661-6596, 1422-0067linking), 2015; 16(7): 15456-15480.
Impact Factor: 3.257
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Dathan NA, Alterio V, Troiano E, Vullo D, Ludwig M, De Simone G, Supuran CT, Monti SM
* Biochemical Characterization Of The Chloroplastic β-Carbonic Anhydrase From Flaveria Bidentis (l. ) "kuntze" (351 visite)
J Enzym Inhib Med Ch (ISSN: 1475-6366, 1475-6374electronic, 1475-6366linking), 2014; 29(4): 500-504.
Impact Factor: 2.332
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Alterio V, Pan P, Parkkila S, Buonanno M, Supuran CT, Monti SM, De Simone G
* The Structural Comparison Between Membrane-Associated Human Carbonic Anhydrases Provides Insights Into Drug Design Of Selective Inhibitors (374 visite)
Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 2014; 101(7): 769-778.
Impact Factor: 2.385
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Rami M, Dubois L, Parvathaneni NK, Alterio V, van Kuijk SJ, Monti SM, Lambin P, De Simone G, Supuran CT, Winum JY
* Hypoxia-targeting carbonic anhydrase IX inhibitors by a new series of nitroimidazole-sulfonamides/sulfamides/sulfamates (478 visite)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2013 Nov 14; 56(21): 8512-8520.
Impact Factor: 5.48
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De Simone G, Alterio V, Supuran CT
* Exploiting the hydrophobic and hydrophilic binding sites for designing carbonic anhydrase inhibitors (382 visite)
Expert Opin Drug Discov (ISSN: 1746-0441), 2013 Jul; 8(7): 793-810.
Impact Factor: 3.467
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Monti SM, Supuran CT, De Simone G
* Anticancer carbonic anhydrase inhibitors: A patent review (2008-2013) (383 visite)
Expert Opin Ther Pat (ISSN: 1354-3776, 1744-7674electronic), 2013 Jun; 23(6): 737-749.
Impact Factor: 3.441
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Alterio V, Di Fiore A, D'Ambrosio K, Supuran CT, De Simone G
* Multiple binding modes of inhibitors to carbonic anhydrases: How to design specific drugs targeting 15 different isoforms? (391 visite)
Chem Rev (ISSN: 0009-2665), 2012 Sep; 112(8): 4421-4468.
Impact Factor: 41.298
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De Simone G, Supuran CT
* (In)organic anions as carbonic anhydrase inhibitors (348 visite)
J Chem Res (ISSN: 0162-0134, 1873-3344, 0162-0134print), 2012 Jun; 111: 117-129.
Impact Factor: 3.197
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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 (338 visite)
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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Di Fiore A, Maresca A, Supuran CT, De Simone G
* Hydroxamate represents a versatile zinc binding group for the development of new carbonic anhydrase inhibitors (320 visite)
Chem Commun (ISSN: 1359-7345, 1364-548x, 1364-548xelectronic), 2012; 48(70): 8838-8840.
Impact Factor: 6.378
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Di Fiore A, Maresca A, Alterio V, Supuran CT, De Simone G
* Carbonic anhydrase inhibitors: X-ray crystallographic studies for the binding of N-substituted benzenesulfonamides to human isoform II (317 visite)
Chem Commun (ISSN: 1359-7345, 1364-548x, 1364-548xelectronic), 2011; 47(42): 11636-11638.
Impact Factor: 6.169
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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 (299 visite)
Bioorganic & Medicinal Chemistry Letters (ISSN: 0960-894x), 2010 Sep 15; 20(16): 4745-4748.
Impact Factor: 2.661
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Alterio V, Monti SM, Truppo E, Pedone C, Supuran CT, De Simone G
* The first example of a significant active site conformational rearrangement in a carbonic anhydrase-inhibitor adduct: The carbonic anhydrase I-topiramate complex (365 visite)
Org Biomol Chem (ISSN: 1477-0520, 1477-0539, 1477-0539electronic), 2010 Sep 7; 8(15): 3528-3533.
Impact Factor: 3.451
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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 (280 visite)
Bioorg Med Chem Lett (ISSN: 0960-894x), 2010 Sep 1; 20(17): 5023-5026.
Impact Factor: 2.661
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Di Fiore A, Monti SM, Innocenti A, Winum J-Y, De Simone G, Supuran CT
* Carbonic anhydrase inhibitors: Crystallographic and solution binding studies for the interaction of a boron-containing aromatic sulfamide with mammalian isoforms I-XV (313 visite)
Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2010 Jun 15; 20(12): 3601-3605.
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 (437 visite)
Curr Med Chem (ISSN: 0929-8673, 1875-533x, 1875-533xelectronic), 2010; 17(15): 1516-1526.
Impact Factor: 4.63
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Supuran CT, Di Fiore A, Alterio V, Monti SM, De Simone G
* Recent advances in structural studies of the carbonic anhydrase family: The crystal structure of human CA IX and CA XIII (401 visite)
Curr Pharm Des Current Pharmaceutical Design (ISSN: 1381-6128, 1873-4286), 2010; 16(29): 3246-3254.
Impact Factor: 4.774
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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 (447 visite)
Eur J Nucl Med (ISSN: 1619-7070, 1619-7089, 0340-6997), 2009 Dec; 36(12): 2093-2102.
Impact Factor: 4.531
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Vitale RM, Alterio V, Innocenti A, Winum JY, Monti SM, De Simone G, Supuran CT
* Carbonic anhydrase inhibitors. Comparison of aliphatic sulfamate/bis- sulfamate adducts with isozymes II and IX as a platform for designing tight-binding, more isoform-selective inhibitors (393 visite)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2009 Oct 8; 52(19): 5990-5998.
Impact Factor: 4.802
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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
* Crystal structure of the catalytic domain of the tumor-associated human carbonic anhydrase IX (479 visite)
P Natl Acad Sci Usa (ISSN: 0027-8424, 1091-6490, 0027-8424print), 2009 Sep 22; 106(38): 16233-16238.
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? (304 visite)
Chem Biol Drug Des Chemical Biology And Drug Design (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 (409 visite)
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
* Biochemical characterization of CA IX, one of the most active carbonic anhydrase isozymes (384 visite)
Jbc Papers (ISSN: 0021-9258, 1083-351x, 0021-9258linking), 2008 Oct 10; 283(41): 27799-27809.
Impact Factor: 5.52
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D'Ambrosio K, Vitale R, Dogne J, Masereel B, Innocenti A, Scozzafava A, De Simone G, Supuran CT
* Ccarbonic Anhydrase Inhibitors: Bioreductive Nitro-Containing Sulfonamides With Selectivity For Targeting The Tumor Associated Isoforms Ix And Xii (443 visite)
J Med Chem (ISSN: 1520-4804, 0022-2623, 0022-2623print), 2008 Jun 12; 51(11): 3230-3237.
Impact Factor: 4.898
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Supuran CT, Di Fiore A, De Simone G
* Carbonic anhydrase inhibitors as emerging drugs for the treatment of obesity (414 visite)
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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Di Fiore A, Pedone C, Antel J, Waldeck H, Witte A, Wurl M, Scozzafava A, Supuran CT, De Simone G
* Carbonic anhydrase inhibitors: the X-ray crystal structure of ethoxzolamide complexed to human isoform II reveals the importance of thr200 and gln92 for obtaining tight-binding inhibitors (361 visite)
Bioorg Med Chem Lett (ISSN: 1464-3405, 0960-894x, 1464-3405electronic), 2008 Apr 15; 18(8): 2669-2674.
Impact Factor: 2.531
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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 (339 visite)
Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2008 Apr 1; 18(7): 2267-2271.
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
* Structure-activity relationships of C-17 cyano-substituted estratrienes as anticancer agents (386 visite)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2008 Mar 13; 51(5): 1295-1308.
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? (361 visite)
Curr Pharm Des Current Pharmaceutical Design (ISSN: 1381-6128, 1873-4286), 2008 Mar; 14(7): 655-660.
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 (333 visite)
Chemmedchem (ISSN: 1860-7179, 1860-7187, 1860-7187electronic), 2008 Mar; 3(3): 473-477.
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 (332 visite)
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 (494 visite)
Nature Reviews Neuroscience (ISSN: 1471-0048), 2007 Oct; 8(10): 766-775.
Impact Factor: 24.52
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Alterio V, De Simone G, Monti SM, Scozzafava A, Supuran CT
* Carbonic anhydrase inhibitors: Inhibition of human, bacterial, and archaeal isozymes with benzene-1, 3-disulfonamides-Solution and crystallographic studies (304 visite)
Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2007 Sep 1; 17(15): 4201-4207.
Impact Factor: 2.604
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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 (311 visite)
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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Di Fiore A, Scozzafava A, Winum JY, Montero JL, Pedone C, Supuran CT, De Simone G
* Carbonic anhydrase inhibitors: binding of an antiglaucoma glycosyl-sulfanilamide derivative to human isoform II and its consequences for the drug design of enzyme inhibitors incorporating sugar moieties (389 visite)
Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2007 Mar 15; 17(6): 1726-1731.
Impact Factor: 2.604
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De Simone G, Supuran CT
* Antiobesity carbonic anhydrase inhibitors (396 visite)
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 (799 visite)
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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Menchise V, De Simone G, Di Fiore A, Scozzafava A, Supuran CT
* Carbonic anhydrase inhibitors: X-ray crystallographic studies for the binding of 5-amino-1, 3, 4-thiadiazole-2-sulfonamide and 5-(4-amino-3-chloro-5-fluorophenylsulfonamido)1, 3, 4-thiadiazole-2-sulfon amide to human isoform II (280 visite)
Bioorganic & Medicinal Chemistry Letters (ISSN: 0960-894x), 2006 Dec 15; 16(24): 6204-6208.
Impact Factor: 2.538
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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 (417 visite)
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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Alterio V, Vitale RM, Monti SM, Pedone C, Scozzafava A, Cecchi A, De Simone G, Supuran CT
* Carbonic anhydrase inhibitors: X-ray and molecular modeling study for the interaction of a fluorescent antitumor sulfonamide with isozyme II and IX (374 visite)
J Am Chem Soc (ISSN: 0002-7863, 0002-2786, 1520-5126), 2006 Jun 28; 128(25): 8329-8335.
Impact Factor: 7.696
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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 (292 visite)
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 (443 visite)
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 (306 visite)
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 (436 visite)
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 (240 visite)
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 (568 visite)
15th World Congress Angiology Rome, 1989; 20(4): 284-284.
Impact Factor: 0
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55 Records (53 escludendo Abstract e Conferenze).
Impact factor totale: 274.918 (269.803 escludendo Abstract e Conferenze).
Impact factor a 5 anni totale: 283.336 (277.832 escludendo Abstract e Conferenze).
Impact factor totale: 274.918 (269.803 escludendo Abstract e Conferenze).
Impact factor a 5 anni totale: 283.336 (277.832 escludendo Abstract e Conferenze).
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