Jean-Yves Winum
2023
186- Ourdjini Z, Kraim K, Winum J-Y, Benoist E, Seridi A. A combined DFT and molecular docking study on novel tricarbonylrhenium(I) complexes bearing mono- and bivalent benzenesulfonamide scaffolds as human carbonic anhydrase IX and XII inhibitors. Journal of Molecular Structure 2023, 1282, 135211.
185- Roy B, Gasca S, Winum J-Y. Chem’Sc@pe: an Organic Chemistry Learning Digital Escape Game. Journal of Chemical Education 2023, 100, 1382-1391.
2022
184- Da Silva Júnior JN, Winum J-Y, Basso A, Gelati L, Moni L, Melo Leite Junior AJ, Mafezoli J, Zampieri D, Serra Oliveira AF, Veja KB, Monteiro AJ. STR120: A Web-Based Board Game for Aiding Students in Review of the Structural Theory of Organic Compounds. Journal of Chemical Education 2022, 99, 3315-3322.
183- Da Silva Júnior JN, Sousa Lima MA, Miranda Nunes F, Melo Leite Junior AJ, Serra Oliveira Alexandre F, de Oliveira Assis DC, Janô Nobre D, Winum J-Y, Jalles Monteiro A, Ferreira de Lima DT. Addition to “Nomenclature Bets: An Innovative Computer-Based Game to Aid Students in the Study of Nomenclature of Organic Compounds─Version 2.0” Journal of Chemical Education 2022, 99, 2208-2212.
182- Da Silva Júnior JN, Zampieri D, Melo Leite Junior AJ, Serra Oliveira Alexandre F, Winum J-Y, Basso A, Jalles Monteiro A, Lima da Silva L. A Virtual Game-Based Tournament to Engage Students in Reviewing Organic Acids and Bases Concepts Journal of Chemical Education 2022, 99, 2190–2197.
181- Merabti A, Roger M, Nguyen C, Nocentini A, Gerbier P, Richeter S, Gary-Bobo M, Supuran CT, Clément S, Winum J-Y.Carbonic Anhydrase Inhibitors Featuring a Porphyrin Scaffold: Synthesis, Optical and Biological Properties. European Journal of Organic Chemistry 2022, 21, e202101538. (Hot article)
180- Anduran E, Lambin P, Dubois L, Winum J-Y. Hypoxia-activated prodrug derivatives of anti-cancer drugs: a patent review 2006-2021. Expert Opinion on Therapeutic Patents. 2022. 32, 1-12.
179- Ismail C, Nocentini A, Supuran CT, Winum J-Y, Gharbi R. 1,5-Benzodiazepines as a platform for the design of carbonic anhydrase inhibitors. Archiv der Pharmazie (Weinheim). 2022, 355, e2100405.
178- Mustafa M, Winum J-Y. The importance of sulfur-containing motifs in drug design and discovery. Expert Opinion on Drug Discovery 2022, 17, 501-512.
2021
177- Aimene Y, Eychenne R, Rodriguez F, Mallet-Ladeira S, Saffon-Merceron N, Winum J-Y, Nocentini A, Supuran CT, Benoist E, Seridi A. Synthesis, Crystal Structure, Inhibitory Activity and Molecular Docking of Coumarins/Sulfonamides Containing Triazolyl Pyridine Moiety as Potent Selective Carbonic Anhydrase IX and XII Inhibitors. Crystals 2021, 11(9), 1076.
176- Da Silva Júnior JN, Esdras de Andrade Uchoa D, Sousa Lima MA, Jalles Monteiro A, Melo Leite Junior AJ, Winum J-Y, Basso A. Addition to “Stereochemistry Game: Creating and Playing a Fun Board Game To Engage Students in Reviewing Stereochemistry Concepts—The Online Version”. Journal of Chemical Education 2021, 98, 3055-3057.
175- Da Silva Júnior JN, Sousa Lima Ma, Silva De Sousa U, Macedo Do Nascimento D, Melo Leite Junior AJ, Benedetti Vega K, Roy B, Winum J-Y. Addition to “Reactions: An Innovative and Fun Hybrid Game to Engage the Students Reviewing Organic Reactions in the Classroom”: Using the Game Remotely during the COVID-19 Pandemic. Journal of Chemical Education 2021, 98, 2735-2737.
174- da Silva Júnior JN, Melo Leite Junior AJ, Winum J-Y, Basso A, Silva de Sousa U, Macedo do Nascimento D, Moura Alves S. HSG400 – Design, implementation, and evaluation of a hybrid board game for aiding chemistry and chemical engineering students in the review of stereochemistry during and after the COVID-19 pandemic. Education for Chemical Engineers 2021, 36, 90-99.
173- Ismail C, Mtiraoui H, Winum J-Y, Msaddek M, Gharbi R. Design, synthesis and photoluminescent studies of new 1,5-benzodiazepines derivatives: Towards new ESIPT compounds. Tetrahedron 2021, 86, 132078.
172- Nocentini A, Angeli A, Carta F, Winum J-Y, Zalubovskis R, Carradori S, Capasso, C, Donald WA, Supuran CT. Reconsidering anion inhibitors in the general context of drug design studies of modulators of activity of the classical enzyme carbonic anhydrase Journal of Enzyme Inhibition and Medicinal Chemistry 2021, 36, 561-580.
171- Winum J-Y, Bernaud L, Filhol, JS. The Hunt for Maya Purple: Revisiting Ancient Pigments Synthesis and Properties. Journal of Chemical Education 2021, 98, 1389-1396.
170- Da Silva Junior JN, Sousa Lima MA, Torres Ávila Pimenta A, Miranda Nunes F, Carvalho Monteiro A, Silva De Sousa U, Melo Leite Junior AJ, Zampieri D, Serra Oliveira Alexandre F, Pacioni NL, Winum J-Y. Design, Implementation, and Evaluation of a Game-based Application for Aiding Chemical Engineering and Chemistry Students to Review the Organic Reactions. Education for Chemical Engineers 2021, 34, 106-114.
169- Angeli A, Carta F, Nocentini A, Winum J-Y, Zalubovskis R, Akdemir A, Onnis V.; Eldehna, W.M., Capasso, C, Simone, GD, Monti SM, Carradori S, Donald WA, Dedhar S, Supuran CT. Perspectives on the Classical Enzyme Carbonic Anhydrase and the Search for Inhibitors. Biophysical Journal 2021, 120, 178-181.
2020
168- Sarnella A, D’avino G, Hill BS, Alterio V, Winum J-Y, Supuran CT, De Simone, G, Zannetti, A. A Novel Inhibitor of Carbonic Anhydrases Prevents Hypoxia-Induced TNBC Cell Plasticity. International Journal Molecular Sciences 2020, 21, 8405.
167- Angeli A, Carta F, Nocentini A, Winum J-Y, Zalubovskis R, Akdemir A, Onnis V.; Eldehna, W.M., Capasso, C, Simone, Gd, Monti SM, Carradori S, Donald Wa, Dedhar S, Supuran CT. Carbonic Anhydrase Inhibitors Targeting Metabolism and Tumor Microenvironment. Metabolites 2020, 10, 412.
166– Da Silva Junior JN, De Sousa Oliveira JM, Winum J-Y, Melo Leite Junior AJ, Serra Oliveira Alexandre F, Macedo Do Nascimento D, Silva De Sousa U, Torres Ávila Pimenta A, Jalles Monteiro A. Interactions 500: Design, Implementation, and Evaluation of a Hybrid Board Game for Aiding Students in the Review of Intermolecular Forces During the COVID-19 Pandemic. Journal of Chemical Education 2020, 97, 4049-4054.
165– Bonardi A, Nocentini A, Cadoni R, Del Prete S, Dumy P, Capasso C, Gratter Pi, Supuran CT, Winum J-Y.Benzoxaboroles: New Potent Inhibitors of the Carbonic Anhydrases of the Pathogenic Bacterium Vibrio cholerae. ACS Medicinal Chemistry Letters 2020, 11, 2277-2284.
164- Da Silva Júnior JN, Sousa Lima Ma, Silva De Sousa U, Macedo Do Nascimento D, Melo Leite Junior AJ, Benedetti Vega K, Roy B, Winum J-Y. Reactions: An Innovative and Fun Hybrid Game to Engage the Students Reviewing Organic Reactions in the Classroom. Journal of Chemical Education 2020, 97, 749-753.
163- Gütschow M, Eynde JJV, Jampilek J, Kang C, Mangoni Aa, Fossa P, Karaman R, Trabocchi A, Scott Pjh, Reynisson J, Rapposelli S, Galdiero S, Winum J-Y, Brullo C, Prokai-Tatrai K, Sharma Ak, Schapira M, Azuma YT, Cerchia L, Spetea M, Torri G, Collina S, Geronikaki A, García-Sosa At, Vasconcelos MH, Sousa ME, Kosalec I, Tuccinardi T, Duarte If, Salvador JAR, Bertinaria M, Pellecchia M, Amato J, Rastelli G, Gomes PAC, Guedes RC, Sabatier JM, Estévez-Braun A, Pagano B, Mangani S, Ragno R, Kokotos G, Brindisi M, González FV, Borges F, Miloso M, Rautio J, Muñoz-Torrero D. Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes-7. Molecules. 2020, 25, 2968.
162- Anduran E, Aspatwar A, Parvathaneni Nk, Suylen D, Bua S, Nocentini A, Parkkila S, Supuran CT, Dubois L, Lambin P, Winum J-Y. Hypoxia-Activated Prodrug Derivatives of Carbonic Anhydrase Inhibitors in Benzenesulfonamide Series: Synthesis and Biological Evaluation. Molecules. 2020, 25, 2347.
161- Gilles A, Frechin L, Natchiar K, Biondani G, Loeffelholz OV, Holvec S, Malaval JL, Winum J-Y, Klaholz BP, Peyron JF. Targeting the Human 80S Ribosome in Cancer: From Structure to Function and Drug Design for Innovative Adjuvant Therapeutic Strategies. Cells 2020, 9, 629.
160- Aspatwar A, Parvathaneni N-K, Barker H, Anduran E, Supuran Ct, Dubois L, Lambin P, Parkilla S, Winum J-Y. Design, synthesis, in vitro inhibition and toxicological evaluation of human carbonic anhydrases I, II and IX inhibitors in 5-nitroimidazole series. Journal of Enzyme Inhibition and Medicinal Chemistry 2020, 35,109-117.
2019
159- Vanden Eynde JJ, Mangoni Aa, Rautio J, Leprince J, Azuma YT, García-Sosa AT, Hulme C, Jampilek J, Karaman R, Li W, Gomes PAC, Hadjipavlou-Litina D, Capasso R, Geronikaki A, Cerchia L, Sabatier JM, Ragno R, Tuccinardi T, Trabocchi A, Winum J-Y, Luque FJ, Prokai-Tatrai K, Spetea M, Gütschow M, Kosalec I, Guillou C, Vasconcelos MH, Kokotos G, Rastelli G, De Sousa ME, Manera C, Gemma S, Mangani S, Siciliano C, Galdiero S, Liu H, Scott PJH, De Los Ríos C, Agrofoglio LA, Collina S, Guedes RC, Muñoz-Torrero D. Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes-6. Molecules. 2019, 25(1). pii: E119.
158- Carta F, Dumy P, Supuran CT, Winum J-Y. Multivalent Carbonic Anhydrases Inhibitors. International Journal of Molecular Sciences 2019, 20, 5352.
157- Langella E, Alterio V, D’ambrosio K, Cadoni R, Winum J-Y, Supuran CT, Monti SM, De Simone G, Di Fiore A. Exploring benzoxaborole derivatives as carbonic anhydrase inhibitors: structural and computational analysis reveals their conformational variability as a tool to increase enzyme selectivity. Journal of Enzyme Inhibition and Medicinal Chemistry2019, 34, 1498-1505.
156- Larcher A, Nocentini A, Supuran C.T., Winum J-Y., Van Der Lee A., Vasseur J-J., Laurencin D, Smietana M. Bis-benzoxaboroles: design, synthesis and biological evaluation as carbonic anhydrase inhibitors. ACS Medicinal Chemistry Letters 2019, 10, 1205-1210.
155- Capasso C, Winum J-Y. Novel method of treating macular degeneration: A patent evaluation (WO2018/107005). Expert Opinion on Therapeutic Patents 2019, 29, 749-752.
154- Richichi B, Spyroulias GA, Winum J-Y, Zalubovskis R. Metalloenzymes as Therapeutic Targets. Current Medicinal Chemistry 2019, 26, 2556-2557.
153- Zalubovskis R, Winum J-Y. Inhibitors of Selected Bacterial Metalloenzymes. Current Medicinal Chemistry 2019, 26, 2690-2714.
152- Bozdag M, Angeli A, Poli G, Tuccinardi T, Selleri S, Winum J-Y, Carta F, Supuran C.T. N-Aryl-N’-ureido-O-sulfamates: Potent and Selective Inhibitors of the Human Carbonic Anhydrase VII Isoform with Neuropathic Pain-Relieving Properties. Bioorganic Chemistry 2019, 89, 103033.
151- Aimene Y, Eychenne R, Mallet-Ladeira S, Saffon N, Winum J-Y, Nocentini A., Supuran CT, Benoist E, Seridi A. Novel Re(I) tricarbonyl coordination compounds based on 2-pyridyl-1,2,3-triazole derivatives bearing a 4-amino-substituted benzenesulfonamide arm: Synthesis, crystal structure, computational studies and inhibitory activity against carbonic anhydrase I, II and IX isoforms. Journal of Enzyme Inhibition and Medicinal Chemistry 2019, 34, 773-782.
150- Rami M, Winum J-Y, Supuran CT, Melnyk P, Yous S. (Hetero)aryl substituted thiazol-2,4-yl scaffold as human carbonic anhydrase I, II, VII and XIV activators. Journal of Enzyme Inhibition and Medicinal Chemistry 2019, 34, 224-229.
2018
149- Aspatwar A, Winum J-Y, Carta F, Supuran CT, Hammaren M, Parikka M, Parkkila S. Carbonic anhydrase inhibitors as novel drugs against mycobacterial β-carbonic anhydrases: An update on in vitro and in vivo studies. Molecules 2018, 23, 2911.
148- De Simone G, Angeli A, Bozdag M, Supuran CT, Winum J-Y, Monti SM, Alterio V. Inhibition of carbonic anhydrases by a substrate analog: benzyl carbamate directly coordinates the catalytic zinc ion mimicking bicarbonate binding. Chemical Communications 2018, 54, 10312-10315.
147- Aspatwar A, Becker Hm, Parvathaneni NK, Hammarena M, Svorjova A, Barker H, Supuran CT, Dubois L, Lambin P, Parikka M, Parkkila S, Winum J-Y. Nitroimidazole based inhibitors DTP338 and DTP348 are safe for zebrafish embryos and efficiently inhibit the activity of human CA IX in Xenopus oocytes. Journal of Enzyme Inhibition and Medicinal Chemistry 2018, 33, 1064-1073.
146- Winum J-Y. Carbonic anhydrase Enzymes for Regulating Mast Cell Hematopoiesis and Type-2 Inflammation: A patent evaluation (WO2017/058370). Expert Opinion on Therapeutic Patents. 2018, 28, 741-743.
145- Nocentini A., Supuran C.T., Winum J-Y. Benzoxaborole compounds for therapeutic uses: a patent review (2010-2018). Expert Opinion on Therapeutic Patents. 2018, 28, 493-504.
144- Nocentini A., Cadoni R., Dumy P., Supuran C.T., Winum J-Y. Carbonic anhydrases from Trypanosoma cruzi and Leishmania donovani chagasi are inhibited by benzoxaboroles. Journal of Enzyme Inhibition and Medicinal Chemistry 2018, 33, 286-289.
143- Imbert V., Nebout M., Mary D., Endou H., Wempe MF., Supuran CT., Winum J-Y., Peyron J-F. Co-Targeting Intracellular Ph And Essential Amino Acid Uptake Cooperates to Induce Cell Death Of T-All/Ll Cells. Leukemia & Lymphoma, 2018, 59, 460-468.
2017
142- Nocentini A., Cadoni R., Del Prete S., Capasso C., Dumy P., Gratteri P., Supuran C.T., Winum J-Y. Benzoxaboroles as efficient inhibitors of the beta-carbonic anhydrases from pathogenic fungi: activity and modelling study. ACS Medicinal Chemistry Letters, 2017, 8, 1194-1198.
141- Kanfar N., Mehdi A., Dumy P., Ulrich S., Winum J-Y. Polyhedral oligomeric silsesquioxane (POSS) bearing glyoxylic aldehyde as clickable platform towards multivalent conjugates. Chemistry : A European Journal, 2017, 23, 17867 – 17869. (hot article + Inside Cover)
140- De Simone, G., Langella, E., Esposito, D., Supuran, C.T., Monti, S.M., Winum, J-Y., Alterio, V. Insights into the binding mode of sulfamates and sulfamides to hCA II: crystallographic studies and binding free energy calculations. Journal of Enzyme Inhibition and Medicinal Chemistry 2017, 32, 1002-1011.
139- Del Prete S., Vullo D., Osman S.M., Alothman Z., Donald W.A., Winum J-Y., Supuran C.T., Capasso C. Anion inhibitors of the b-carbonic anhydrase from the pathogenic bacterium responsible of tularemia, Francisella tularensis. Bioorganic and Medicinal Chemistry 2017, 25, 4800-4804.
138- Kanfar N., Tanc M., Dumy P., Supuran CT., Ulrich S., Winum J-Y. Effective Access to Multivalent Inhibitors of Carbonic Anhydrases Promoted by Peptide Bioconjugation. Chemistry: A European Journal, 2017, 23, 6788-6794 (hot article + Inside Cover)
137- Kohler S., Ouahrani-Bettache S., Winum J-Y. Brucella suis carbonic anhydrases and their inhibitors: towards alternative antibiotics? Journal of Enzyme Inhibition and Medicinal Chemistry 2017, 32, 683-687.
136- Van Kujik S., Parvathaneni N-K., Niemans R., Van Gisbergen MW., Carta F., Vullo D., Pastorekova S., Yaromina A., Supuran CT., Dubois L., Winum J-Y., Lambin P. New approach of delivering cytotoxic drugs towards CAIX expressing cells: A concept of dual-target drugs. European Journal of Medicinal Chemistry 2017, 127, 691-702.
2016
135- Winum J-Y. Synthesis and composition of amino acid linking groups conjugated to compounds used for the targeted imaging of tumors: a patent evaluation of US20160011199A1. Expert Opinion on Therapeutic Patents 2016, 26, 1223-1226.
134- Alterio V., Cadoni R., Esposito D., Vullo D., Di Fiore A., Monti SM., Caporale A., Ruvo M., Sechi M., Dumy P., Supuran CT., De Simone G., Winum J-Y. Benzoxaborole as a New Chemotype for Carbonic Anhydrase Inhibition. Chemical Communications 2016, 52, 11983-11986.
133- Di Fiore A., De Simone G., Alterio V., Riccio V., Winum J-Y., Carta F., Supuran C-T. The anticonvulsant sulfamide JNJ-26990990 and its S, S – dioxide analog strongly inhibit carbonic anhydrases: kinetic and X-ray crystallographic studies. Organic & Biomolecular Chemistry 2016, 14, 4853-4858.
2015
132- Kanfar N., Bartolami E., Zelli R., Marra A., Winum J-Y., Ulrich S., Dumy P. Emerging trends in enzyme inhibition by multivalent nanoconstructs. Organic & Biomolecular Chemistry 2015, 13, 9894-9906.
131- Dubois LJ., Niemans R., Van Kuijk SJ., Panth KM., Parvathaneni NK., Peeters SG., Zegers CM., Rekers NH., Van Gisbergen MW., Biemans R., Lieuwes NG., Spiegelberg L., Yaromina A., Winum J-Y., Vooijs M., Lambin P. New ways to image and target tumour hypoxia and its molecular responses. Radiotherapy and Oncology 2015, 116, 352-357.
130- Supuran CT., Winum J-Y. Carbonic Anhydrase IX Inhibitors in Cancer Therapy: an Update. Future Medicinal Chemistry 2015, 7, 1407-14.
129- Di Fiore A., Vergara A., Caterino M., Alterio V., Monti S., Ombouma J., Dumy P., Vullo D., Supuran CT., Winum J-Y., De Simone, G. Hydroxylamine-O-sulfonamide is a versatile lead compound for the development of carbonic anhydrase inhibitors. Chemical Communications 2015, 51, 11519-22.
128- Ombouma J., Vullo D., Dumy P., Supuran Ct., Winum J-Y. Carbonic Anhydrase Glycoinhibitors belonging to the Aminoxysulfonamide Series. ACS Medicinal Chemistry Letters 2015, 6, 819-21.
127- Ward C., Meehan J., Mullen P., Supuran CT., Dixon JM., Thomas JS., Winum J-Y., Lambin P., Dubois L., Pavathaneni NK., Jarman EJ., Renshaw L., Um I., Kay C., Kunkler LH., Harrison DJ., Langdon SP. Evaluation of Carbonic Anhydrase IX as a Therapeutic Target for Inhibition of Breast Cancer Invasion and Metastasis Using a Series of in vitro Breast Cancer Models. Oncotarget 2015, 6, 24856-24870.
126- Carta F., Osman SM., Vullo D., Gullotto A., Winum J-Y., Alothman Z., Masini E., Supuran CT. Poly(amidoamine) Dendrimers with Carbonic Anhydrase Inhibitory Activity and Antiglaucoma Action. Journal of Medicinal Chemistry 2015,58, 4039-4045.
125- Touisni N., Kanfar N., Ulrich S., Dumy P., Supuran CT., Mehdi A., Winum J-Y. Fluorescent silica nanoparticles with multivalent inhibitory effects towards carbonic anhydrases. Chemistry: a European Journal 2015, 21, 10306-10309. (Hot article + front cover + cover profile).
124- Supuran CT., Winum J-Y. Designing carbonic anhydrase inhibitors for the treatment of breast cancer. Expert Opinion on Drug Discovery 2015, 10, 591-597.
123- Ombouma J., Vullo D., Kohler S., Dumy P., Supuran Ct., Winum J-Y. N-Glycosyl-N-Hydroxysulfamides as Potent Inhibitors of Brucella suis Carbonic Anhydrases. Journal of Enzyme Inhibition and Medicinal Chemistry 2015, 30, 1010-1012.
122- Riafrecha Le., Vullo D., Ouahrani-Bettache S., Köhler S., Dumy P., Winum J-Y., Supuran Ct., Colinas Pa. Inhibition of β-carbonic anhydrases from Brucella suis with C-cinnamoyl glycosides incorporating the phenol moiety. Journal of Enzyme Inhibition and Medicinal Chemistry 2015, 30, 1017-1020.
121- Winum J-Y., Supuran CT. Recent advances in the discovery of zinc binding motifs for the development of carbonic anhydrase inhibitors. Journal of Enzyme Inhibition and Medicinal Chemistry 2015, 30, 321-324.
120- Sasso E., Vitale M., Monteleone F., Boffo Fl., Santoriello M., Sarnataro D., Garbi C., Sabatella M., Crifò B., Paolella LA., Minopoli G., Winum J-Y., Zambrano N. Binding of carbonic anhydrase IX to 45s rDNA genes is prevented by exportin-1 in hypoxic cells BioMed Research International. 2015, Volume 2015, Article ID 674920, 10 pages.
2014
119- Turtaut F., Lopez M., Ouahrani-Bettache S., Kohler S., Winum J-Y. Oxo- and thiooxo-imidazo[1,5-c] pyrimidine molecule library: beyond their interest in inhibition of Brucella suis histidinol dehydrogenase, a powerful protection tool in the synthesis of histidine analogues. Bioorganic and Medicinal Chemistry Letters 2014, 24, 5008-5010.
118- Ombouma J., Vullo D., Supuran CT., Winum J-Y. Ferrier sulfamidoglycosylation of glycals catalyzed by nitrosononium tetrafluoroborate: towards new carbonic anhydrase glycoinhibitors. Bioorganic and Medicinal Chemistry 2014, 22, 6353-6359.
117- Saada Mc., Vullo D., Montero J-L., Scozzafava A., Supuran CT., Winum J-Y. Mono and Di-Halogenated Histamine, Histidine and Carnosine Derivatives are Potent Carbonic Anhydrase I, II, VII, XII and XIV Activators. Bioorganic and Medicinal Chemistry 2014, 22, 4752-8.
116– Abdelarhim MY., Tanc AM., Winum J-Y., Supuran CT., Barboiu M. Dominant behaviours in the expression of human of Carbonic Anhydrase hCA I activity. Chemical Communications 2014, 50, 8043-8046.
115– Nasr G., Cristian A., Barboiu M., Vullo D., Winum J-Y., Supuran Ct. Carbonic anhydrase inhibitors. Inhibition of human cytosolic isoforms I and II with (reduced) Schiff’s bases incorporating sulfonamide, carboxylate and carboxymethyl moieties. Bioorganic and Medicinal Chemistry 2014, 22, 2867-74.
114– D’ambrosio K., Lopez M., Dathan N., Ouahrani-Bettache S., Köhler S., Ascione G., Monti S., Winum J-Y., De Simone G. Structural basis for the rational design of new antibrucella agents: the crystal structure of the C366S mutant of L-histidinol dehydrogenase from Brucella suis. Biochimie 2014, 97, 114-120.
113– Hanif M., Chohan Zh., Winum J-Y., Akhtar J. Metal-based carboxamide-derived compounds endowed with antibacterial and antifungal activity. Journal of Enzyme Inhibition and Medicinal Chemistry 2014, 29, 517-26.
2013
112– Rami M., Dubois L., Parvathaneni Nk., Alterio V., Van Kujik S., Monti S., Lambin P., De Simone G., Supuran CT., Winum J-Y. Hypoxia-targeting Carbonic Anhydrase IX inhibitors by a new series of nitroimidazole-sulfonamide /sulfamide/ sulfamate. Journal of Medicinal Chemistry, 2013, 56, 8512-8520.
111– Dubois L., Peeters Sg., Van Kuijk Sj., Yaromina A., Lieuwes Ng., Saraya R., Biemans R., Rami M., Parvathaneni Nk., Vullo D., Vooijs M., Supuran CT., Winum J-Y., Lambin P. Targeting carbonic anhydrase IX by nitroimidazole based sulfamides enhances the therapeutic effect of tumor irradiation: A new concept of dual targeting drugs. Radiotherapy and Oncology 2013, 108, 523-528.
110- Saada Mc., Ombouma J., Montero J-L., Supuran CT., Winum J-Y. Thiol-ene click chemistry for the synthesis of highly effective glycosyl sulfonamide carbonic anhydrase inhibitors. Chemical Communications, 2013, 49, 5699-701.
109- Belfaragui M., Seridi A., Winum J-Y., Abdaoui M., Kadri M. A spectrophotometric and thermodynamic study of the charge-transfer complexes of N-aryl-N’-isopropyloxycarbonylsulfamides with DDQ and TCNE. Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy 2013, 108, 55-61.
108- Capasso C., Winum J-Y. Novel antibody to a carbonic anhydrase (WO2011138279). Expert Opinion on Therapeutic Patents. 2013, 23, 757-760.
107- Winum J-Y., Colinas P., Supuran C.T. Glycosidic carbonic anhydrase IX inhibitors: a sweet approach against cancer. Bioorganic and Medicinal Chemistry 2013, 21, 1419-1426.
106- Lock F.E., Mcdonald P., Lou Y., Ostlund C., Aparicio S., Winum J-Y., Supuran C.T., Dedhar S. Targeting carbonic anhydrase IX depletes breast cancer stem cells within the hypoxic niche. Oncogene 2013, 32, 5210–5219.
105- Bonneau A., Maresca A., Winum J-Y., Supuran C.T. Metronidazole-coumarin conjugates and 3-cyano-7-hydroxy-coumarin act as isoform-selective carbonic anhydrase inhibitors. Journal of Enzyme Inhibition and Medicinal Chemistry 2013,28, 397-401.
2012
104- Winum J-Y., Maresca A., Carta F., Scozzafava A., Supuran C.T. Polypharmacology of sulfonamide: Pazopanib, a multitargeted receptor tyrosine kinase inhibitor in clinical use, potently inhibits several mammalian carbonic anhydrases. Chemical Communications, 2012, 48, 8177-8179. (Hot article + Cover Page).
103- D’ambroso K., Smaine F-Z., Carta F., De Simone G., Winum J-Y., Supuran C.T. Development of potent carbonic anhydrase inhibitors incorporating both sulfonamide and sulfamide groups. Journal of Medicinal Chemistry, 2012, 55, 6776-6783.
102- Winum J-Y., Carta F., Ward C., Mullen P., Harrison D., Langdon S., Cecchi A., Scozzafava A., Kunkler I., Supuran C.T. Ureido-substituted sulfamates with potent carbonic anhydrase IX inhibitory and antitumor activities. Bioorganic and Medicinal Chemistry Letters 2012, 22, 4681-4685.
101- Gieling R.G., Babur M., Mamnani L., Burrows N., Telfer B.A., Carta F., Winum J-Y., Scozzafava A., Supuran C.T., Williams K.J. Anti-metastatic effect of sulfamate carbonic anhydrase IX inhibitors in breast carcinoma xenografts. Journal of Medicinal Chemistry, 2012, 55, 5591-5600.
100- Balboni G., Congiu C., Onnis V., Maresca A., Scozzafava A., Winum J-Y., Supuran C.T. Flavones and structurally related 4-chromenones inhibit carbonic anhydrases by a different mechanism of action compared to coumarins. Bioorganic and Medicinal Chemistry Letters 2012, 22, 3063-3066.
99– Lopez M., Kohler S., Winum J-Y. Zinc metalloenzymes as new targets against the bacterial pathogen Brucella. Journal of Inorganic Biochemistry 2012, 111, 138-145. (Invitation pour le numéro spécial en l’honneur du Pr. Bert Vallee).
98– Maresca A., Scozzafava A., Kohler S., Winum J-Y., Supuran C.T. Inhibition of the beta-carbonic anhydrases from the bacterial pathogen Brucella suis with inorganic anions. Journal of Inorganic Biochemistry 2012, 110, 36-39.
97- McDonald P., Winum J-Y., Supuran C.T., Dedhar S. Recent Developments in Targeting Carbonic Anhydrase IX for Cancer Therapeutics. Oncotarget, 2012, 3, 84-97.
2011
96- Touisni N., Maresca A., Mcdonald P., Yuanmei L., Scozzafava A., Dedhar S., Winum J-Y., Supuran C.T. Glycosyl coumarin carbonic anhydrase IX and XII inhibitors strongly attenuate the growth of primary breast tumors. Journal of Medicinal Chemistry 2011, 54, 8271-8277.
95- Turtaut F., Ouahrani-Bettache S., Montero J-L., Kohler S., Winum J-Y. Synthesis and biological evaluation of a new class of anti-Brucella compounds targeting histidinol dehydrogenase: a-O-arylketones and a-S-arylketones derived from histidine. MedChemComm. 2011, 2, 995-1000.
94– Rami M., Innocenti A., Montero J-L., Scozzafava A., Winum J-Y., Supuran C.T. Synthesis of rhodamine B – benzenesulfonamide conjugates and their inhibitory activity against human a- and bacterial/fungal b-carbonic anhydrases. Bioorganic and Medicinal Chemistry Letters 2011, 21, 5210-5213.
93- Saada M.C., Vullo D., Montero J-L., Scozzafava A., Winum J-Y., Supuran C.T. Carbonic anhydrase I and II activation with mono- and dihalogenated histamine derivatives. Bioorganic and Medicinal Chemistry Letters 2011, 21, 4884-4887.
92- Rami M., Maresca, A., Smaine F-Z., Montero J-L., Scozzafava A., Winum J-Y., Supuran C.T. Sulfonamides incorporating boroxazolidone moieties are potent inhibitors of the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII. Bioorganic and Medicinal Chemistry Letters 2011, 21, 2975-2979.
91- Lou Y., Mcdonald P.C., Oloumi A., Chia S., Ostlund C., Ahmadi A., Kyle A., Auf Dem Keller U., Leung S., Huntsman D., Clarke B., Sutherland B.W., Waterhouse D., Bally M., Roskelley C., Overall C.M., Minchinton A., Pacchiano A., Carta F., Touisni N., Winum J-Y., Supuran C.T., Dedhar S. Targeting Tumor Hypoxia: Suppression of Breast Tumor Growth and Metastasis by Novel Carbonic Anhydrase IX Inhibitors. Cancer Research 2011, 71, 3364-3376.
90- Abdo M.R., Joseph P., Mortier J., Turtaut F., Montero J-L., Masereel B., Kohler S., Winum J-Y. Anti-virulence Strategy against Brucella suis: Synthesis, Biological Evaluation and Molecular Modeling of Selective Histidinol Dehydrogenase Inhibitors. Organic & Biomolecular Chemistry 2011, 9, 3681-3690.
89- Saada M.C., Montero J-L., Vullo D., Scozzafava A., Winum J-Y., Supuran C.T. Carbonic anhydrase activators: gold nanoparticles coated with derivatized histamine, histidine and carnosine show enhanced activatory effects on several mammalian isoforms. Journal of Medicinal Chemistry 2011, 54, 1170-1177.
88- Joseph P., Bettache S., Montero J-L., Nishimori I., Minakuchi T., Vullo D., Scozzafava A., Winum J-Y., Kohler S., Supuran C.T. A new b-carbonic anhydrase from Brucella suis, its cloning, characterization, and inhibition with sulfonamides and sulfamates, leading to impaired pathogen growth. Bioorganic and Medicinal Chemistry 2011, 19, 1172-1178.
2010
87- Winum J-Y., Kohler S., Supuran C.T. Brucella carbonic anhydrases: New targets for designing anti-infective agents. Current Pharmaceutical Design 2010, 16, 3310-3316.
86- Di Fiore A., Monti S.M., Innocenti A., Winum J-Y., De Simone G., Supuran C.T. Carbonic anhydrase inhibitors. X-ray crystallographic and solution binding studies for the interaction of a boron containing aromatic sulfamide with mammalian isoforms I-XV. Bioorganic and Medicinal Chemistry Letters 2010, 20, 3601-3605.
85- Rami M., Montero J-L., Dubois L., Lambin P., Scozzafava A., Vullo A., Winum J-Y., Supuran C.T. Carbonic Anhydrase Inhibitors: Gd(III) complexes of DOTA- and TETA- sulfonamide conjugates targeting the tumor associated carbonic anhydrase isozymes IX and XII. New Journal of Chemistry 2010, 34, 2139-2144.
84- Vullo D., Nishimori I., Scozzafava A., Kohler S., Winum J-Y., Supuran C.T. Inhibition studies of a b-carbonic anhydrase from Brucella suis with a series of water soluble glycosyl sulfanilamide. Bioorganic and Medicinal Chemistry Letters 2010, 20, 2178-2182.
83- Joseph P., Turtaut F., Bettache S., Montero J-L., Nishimori I., Minakuchi T., Vullo D., Scozzafava A., Kohler S., Winum J-Y., Supuran C.T. Cloning, characterization and inhibition studies of a b-carbonic anhydrase from Brucella suis. Journal of Medicinal Chemistry 2010, 53, 2277-2285.
2009
82- Winum J-Y., Montero J-L., Vullo D., Supuran C.T. Carbonic anhydrase inhibitors: glycosyl sulfanilamides are the first subnanomolar inhibitors of the human secreted isoform VI. Chemical Biology & Drug Design 2009, 74, 636-639.
81- Seridi A., Akkari H., Winum J-Y., Benard-Rocherulle P., Abdaoui M. tert-butyl N-[N,N-bis(2-chloroethyl)-sulfamoyl]-N-(2-chloroethyl)carbamate. Acta Crystallographica 2009, 65, 02543-02544.
80- Nasr G., Petit E., Supuran C.T., Winum J-Y., Barboiu M. Dynamic combinatorial libraries in the presence of human carbonic anhydrase: towards hCA II isozyme-specific inhibitors. Bioorganic and Medicinal Chemistry Letters 2009, 19, 6014-6017.
79- Vitale R.M., Alterio V., Innocenti A., Winum J-Y., Monti S.M., De Simone G., Supuran C.T. 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. Journal of Medicinal Chemistry 2009, 52, 5990-5998.
78- Nasr G., Petit E., Vullo D., Winum J-Y., Supuran C.T., Barboiu M. Carbonic anhydrase-encoded dynamic constitutional libraries: towards the discovery of isozyme-specific inhibitors. Journal of Medicinal Chemistry 2009, 52, 4853-4859.
77- Winum J-Y., Innocenti A., Vullo D., Montero J-L., Supuran C.T. Carbonic anhydrase inhibitors. Fluorinated phenyl sulfamates show strong inhibitory activity and selectivity for the inhibition of the tumor-associated isozymes IX and XII over the cytosolic ones I and II. Bioorganic and Medicinal Chemistry Letters 2009, 19, 5082-5085.
76- Innocenti, A., Winum J-Y., Hall R.A., Schlicker, C., Mühlschlegel F.A., Scozzafava A., Steegborn C., Supuran C.T. Carbonic anhydrase inhibitors. Inhibition of the fungal b-carbonic anhydrases from Candida albicans and Cryptococcus neoformans with boronic acids. Bioorganic and Medicinal Chemistry Letters 2009, 19, 2642-2645.
75- Winum J-Y., Innocenti A., Scozzafava A., Montero J-L., Supuran C.T. Carbonic anhydrase inhibitors. Inhibition of the human cytosolic isoforms I and II and transmembrane, tumor-associated isoforms IX and XII with boronic acids. Bioorganic and Medicinal Chemistry 2009, 17, 3649-3652.
74- Abdo M-R., Vullo D., Saada M-C., Montero J-L, Scozzafava A., Winum J-Y., Supuran C.T. Carbonic anhydrase activators: Activation of human isozymes I, II and IX with phenylsulfonylhydrazido L-histidine derivatives. Bioorganic andMedicinal Chemistry Letters 2009, 19, 2440-2443.
73- Winum J-Y., Scozzafava A., Montero J-L. Supuran C.T. Inhibition of carbonic anhydrase IX: a new strategy against cancer. Anti-Cancer Agents in Medicinal Chemistry 2009, 9, 693-702.
72- Winum J-Y., Poulsen S-A., Supuran C.T. Therapeutic Applications of glycosidic carbonic anhydrase inhibitors. Medicinal Research Reviews 2009, 29, 419-435.
71- Buissiere A., Barragan-Montero V., Winum J-Y., Montero J-L. Expeditious stereoselective synthesis of L-iminosugars via a Mitsunobu reaction. Synlett 2009, 6, 978-980.
2008
70- Stiti M., Cecchi A., Rami M., Abdaoui M., Barragan-Montero V., Scozzafava A., Guari Y., Winum J-Y., Supuran C.T. Carbonic anhydrase inhibitor coated gold nanoparticle selectively inhibit the tumor-associated isoform IX over the cytosolic ubiquitous isozymes I and II. Journal of American Chemical Society 2008, 130, 19130-19131.
69– Smaine F-Z., Pacchiano F., Rami M., Barragan-Montero V., Vullo D., Scozzafava A., Winum J-Y., Supuran C.T. Carbonic anhydrase inhibitors: 2-substituted-1,3,4-thiadiazole-5-sulfamides act as powerful and selective inhibitors of the mitochondrial isozymes VA and VB over the cytosolic and membrane-associated carbonic anhydrase I, II and IV. Bioorganic and Medicinal Chemistry Letters 2008, 18, 6332-6335.
68- Rami M., Cecchi A., Montero J-L., Innocenti A., Vullo D., Scozzafava A, Winum J-Y., Supuran C.T. Carbonic anhydrase inhibitors. Design of membrane-impermeant copper(II) complexes of DTPA-, DOTA- and TETA-tailed sulfonamides targeting the tumor-associated transmembrane isoforme IX. ChemMedChem 2008, 3, 1780-1788.
67- Winum J-Y., Köhler S., Scozzafava A., Montero J-L. Supuran C.T. Targeting bacterial metalloenzymes: a new strategy for the development of anti-infective agents. Anti-infective Agents in Medicinal Chemistry 2008, 7, 169-179.
66- Cecchi A., Ciani L., Winum J-Y., Montero J-L., Scozzafava A., Ristori S., Supuran C.T. Carbonic anhydrase inhibitors. Design of spin-labeled sulfonamides incorporating TEMPO moieties as probes for cytosolic or transmembrane isozymes. Bioorganic and Medicinal Chemistry Letters 2008, 18, 3475-3480.
65- Winum J-Y., Rami M., Scozzafava A., Montero J-L. Supuran C.T. Carbonic anhydrase IX: a new druggable target for the design of antitumor agents. Medicinal Research Reviews 2008, 28, 445-463.
64- Abdo M.R., Joseph P., Boigegrain R.A, Liautard J-P., Montero J-L, Kohler S., Winum J-Y. Brucella suis histidinol dehydrogenase: Synthesis and inhibition studies of substituted N-L-histidinylphenylsulfonyl hydrazide. Journal of Enzyme Inhibition and Medicinal Chemistry 2008, 23, 357-361.
63- Winum J-Y., Scozzafava A., Montero J-L. Supuran C.T. Design of zinc binding function for carbonic anhydrase inhibitors. Current Pharmaceutical Design 2008, 14, 615-621.
62- Rami M., Winum J-Y., Innocenti A., Montero J-L., Scozzafava A., Supuran C.T. Carbonic anhydrase inhibitors. Copper (II) complexes of polyamino-polycarboxylamido aromatic/heterocyclic sulfonamides are very potent inhibitors of the tumor associated isoforms IX and XII. Bioorganic and Medicinal Chemistry Letters 2008, 18, 836-841.
2007
61- Winum J-Y. Carbonic anhydrase IX inhibitors: Fluorescent sulfonamides as therapeutic and diagnostic agents.Expert Opinion in Therapeutic Patents 2007, 17, 1393-1396.
60- Nessaiba M., Abdaoui M., Djahoudi A.G., Kadri M., Winum J-Y. Synthesis of substituted N-aryl-N’-sulfamoyl-oxazolidin-2-ones with potential antibacterial activity. Recent Patents Anti-Infectives Drug Discovery 2007, 2, 131-139.
59- Smaine F-Z, Winum J-Y., Montero J-L., Vullo D., Regainia Z., Scozzafava A., Supuran C.T. Carbonic anhydrase inhibitors. Selective inhibition of the extracellular, tumor-associated isoforms IX and XII over the cytosolic ones I and II with glycosylthioureido-sulfonamides. Bioorganic and Medicinal Chemistry Letters 2007, 17, 5096-5100.
58- Joseph P., Abdo M-R., Boigegrain R-A., Montero J-L., Winum J-Y., Kohler S. Targeting of the virulence factor histidinol dehydrogenase of Brucella suis by histidinol analogues results in inhibition of intramacrophagic multiplication of the pathogen. Antimicrobial Agents and Chemotherapy 2007, 51, 3752-3755.
57- Abdo M.R., Joseph P., Boigegrain R.A, Liautard J-P., Montero J-L, Kohler S., Winum J-Y. Brucella suis histidinol dehydrogenase: Synthesis and inhibition studies of a series of substituted benzylic ketones derivated from histidine. Bioorganic and Medicinal Chemistry 2007, 15, 4427-4433.
56- Winum J-Y., Thiry A., El Cheikh K., Dogne J-M., Montero J-L., Vullo D., Scozzafava A., Masereel B., Supuran C-T. Carbonic Anhydrase Inhibitors. Inhibition of isoforms I, II, IV, VA, VII, IX and XIV with sulfonamides incorporating fructopyranose-thioureido tails. Bioorganic and Medicinal Chemistry Letters 2007, 17, 2685-2691.
55- Temperini C., Winum J-Y., Montero J-L., Scozzafava A., Supuran C-T. Carbonic Anhydrase Inhibitors. The X-ray crystal structure of the adduct of N-hydroxysulfamide with isozyme II explains why this new zinc binding function is effective in the design of potent inhibitors. Bioorganic and Medicinal Chemistry Letters 2007, 17, 2795-2801.
54- Di Fiore A., Supuran C.T., Winum J-Y., Montero J-L., Pedone C., Scozzafava A., 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. Bioorganic and Medicinal Chemistry Letters 2007, 17, 1726-1731.
53- Winum J-Y., Scozzafava A., Montero J-L. Supuran C.T. Metal binding functions in the design of carbonic anhydrase inhibitors. Current Topics in Medicinal Chemistry 2007, 7, 835-848.
2006
52– Winum J-Y., Temperini C., El Cheikh K., Innocenti A., Vullo D., Ciattini S., Montero J-L., Scozzafava A., Supuran C.T. Carbonic anhydrase inhibitors: clashing with Ala65 as a means for designing inhibitors with low affinity for the ubiquitous isozyme II, exemplified by the crystal structure of the topiramate sulfamide analogue. Journal of Medicinal Chemistry 2006, 49, 7024-7031.
51– Seridi A., Winum J-Y., Kadri M., Abdaoui M., Montero J-L. Study on the decomposition of 2-chloroethylnitrososulfamides (CENS) in serum by HPLC on-line solid phase extraction. Archiv der Pharmazie 2006, 339, 521-526.
50– De Simone G, Vitale R.M., Di Fiore A., Pedone C., Scozzafava A., Montero J-L., Winum J-Y., Supuran C.T. Carbonic anhydrase inhibitors: Hypoxia-activatable sulfonamides incorporating disulfide bonds that target the tumor-associated isoform IX. Journal of Medicinal Chemistry 2006, 49, 5544-5551.
49– Hanson J., Reynaud D., Qiao N., Devel P., Moray A-L, Renard J-F., Kelley L.P., Winum J-Y., Montero J-L., Kinsella B., Pirotte B., Pace-Asciak Cr., Dogne J-M. Synthesis and pharmacological evaluation of novel nitrobenzenic thromboxane modulators as anti-platelet agents acting on both the alpha and beta isoforms of the human thromboxane receptor. Journal of Medicinal Chemistry 2006, 49, 3701-3709.
48- Winum J-Y., Cecchi A., Seridi A., Scozzafava A., Montero J-L. Supuran C.T. Carbonic anhydrase inhibitors. N-cyanomethylsulfonamide – A new zinc binding group in the design of inhibitors targeting cytosolic and membrane-anchored isoforms. Journal of Enzyme Inhibition and Medicinal Chemistry 2006, 21, 477-481.
47– Winum J-Y., Montero J-L., Scozzafava A., Supuran C.T. New zinc binding motifs in the design of selective carbonic anhydrase inhibitors. Mini-Reviews in Medicinal Chemistry 2006, 6, 921-936.
46– Winum J-Y., Montero J-L., Scozzafava A., Supuran C.T. Therapeutic potential of sulfamide as enzyme inhibitors. Medicinal Research Reviews 2006, 26, 767-792.
45– Khettache N., Bendjeddou A., Berredjem M., Regainia Z., Montero J-L, Menut C., Aouf N-E., Winum J-Y. Efficient synthesis of chiral 1,1’-sulfonyl bisaziridine. Synthetic Communications 2006, 36, 2299-2305.
44– Seridi A., Kadri M., Abdaoui M., Winum J-Y., Montero J-L. Kinetic investigation on aqueous decomposition of 2-chloroethylnitrososulfamide (CENS). Bioorganic and Medicinal Chemistry Letters 2006, 16, 1021-1027.
43– Winum J-Y., Montero J-L., Scozzafava A., Supuran C.T. The sulfamide motif in the design of enzyme inhibitors. Expert Opinion in Therapeutic Patents 2006, 16, 27-47.
2005
42– Barragan V., Winum J-Y., Moles J-P., Juan E., Montero J-L. Isocannabinoid and cholesterol derivatized surfactants for liposomal targeting of keratinocytes and skin. European Journal of Medicinal Chemistry 2005, 40, 1022-1029.
41- Winum J-Y., Cecchi A., Montero J-L., Innocenti A., Scozzafava A., Supuran C.T. Carbonic Anhydrase inhibitors. Synthesis and inhibition of cytosolic/tumor associated carbonic anhydrase isozymes I, II and IX with boron-containing sulfonamides, sulfamides and sulfamates: towards agents for boron neutron capture therapy of hypoxic tumors. Bioorganic and Medicinal Chemistry Letters 2005, 15, 3302-3306.
40- Garaj V, Puccetti L, Fasolis G, Winum J-Y, Montero J-L, Scozzafava A, Vullo D, Innocenti A, Supuran C-T. Carbonic anhydrase inhibitors: novel sulfonamide incorporating 1,3,5-triazine moieties as inhibitors of the cytosolic and tumor-associated carbonic anhydrase isozymes I, II and IX. Bioorganic and Medicinal Chemistry Letters 2005, 15, 3102-3108.
39– Cecchi A., Hulikova A., Pastorek J., Pastorekova S., Scozzafava A., Winum J-Y., Montero J-L., Supuran C.T. Carbonic Anhydrase Inhibitors. Sulfonamides inhibit isozyme IX mediated acidification of hypoxic tumors. Fluorescent sulfonamides design as probes of membrane-bound carbonic anhydrase isozymes involvement in tumorigenesis. Journal of Medicinal Chemistry 2005, 48, 4834-4841.
38– Puccetti L, Fasolis A, 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. Bioorganic and Medicinal Chemistry Letters 2005, 15, 2359-2364.
37– Winum J-Y, Innocenti A, Nasr J, Montero J-L, Scozzafava A, Supuran C-T. Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, IX and XII with N-hydroxysulfamides – A new zinc binding function in the design of inhibitors. Bioorganic and Medicinal Chemistry Letters 2005, 15, 2353-2358.
36– Kadri M, Djemil R, Abdaoui M, Winum J-Y, Coutrot F, Montero J-L. Inclusion complexes of N-sulfamoyloxazolidinones with b-cyclodextrin. Bioorganic and Medicinal Chemistry Letters 2005, 15, 889-894.
35– Winum J-Y., Innocenti A., Gagnard V., Montero J-L., Scozzafava A., Supuran C.T. Carbonic Anhydrase Inhibitors. Interaction of isozymes I, II, IV, V and IX with organic phosphates and phosphonates. Bioorganic and Medicinal Chemistry Letters 2005, 15, 1683-1686.
34– Winum J-Y. Carbonic Anhydrase Inhibitors: CA IX selective inhibitors incorporating aromatic or heterocyclic sulfonamide. Expert Opinion in Therapeutic Patents 2005, 15, 233-236.
33– Winum J-Y., Pastorekova S., Jakubickova L., Montero J-L., Scozzafava A., Pastorek J., Vullo D., Innocenti A., Supuran C.T. Carbonic Anhydrase Inhibitors: Synthesis and Inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II and IX with bis-sulfamates. Bioorganic and Medicinal Chemistry Letters 2005, 15, 579-584.
32– Winum J-Y., Dogne J-M., Casini A., De Leval X., Montero J-L., Scozzafava A., Vullo D., Innocenti A., Supuran C.T. Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/membrane-associated carbonic anhydrase isozymes I, II and IX with sulfonamide incorporating hydrazine moieties. Journal of Medicinal Chemistry 2005, 48, 2121-2125.
31– Winum J-Y., Montero J-L., Scozzafava A., Supuran C.T. Sulfamates and their therapeutic potential. Medicinal Research Reviews 2005, 25, 186-228.
2004
30– Julemont F., De Leval X., Damas J., Michaux C., Winum J-Y., Montero J-L., Dogne J-M., Pirotte B. Design, synthesis and pharmacological evaluation of pyridinic analogues of nimesulide as COX-2 selective inhibitors. Journal of Medicinal Chemistry 2004, 47, 6749-6750.
29– 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-isothiocyanatobenzolamide. Bioorganic and Medicinal Chemistry Letters 2004, 14, 5775-5780.
28– Garaj V., Puccetti L., Fasolis G., Winum J-Y., Montero J-L., Scozzafava A., Vullo D., Innocenti A., Supuran C.T. Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II and IX with sulfonamides incorporating 1,2,4-triazine moieties. Bioorganic and Medicinal Chemistry Letters 2004, 14, 5427-5433.
27- Bonnac L., Innocenti A., Winum J-Y., Casini A., Montero J-L., Scozzafava A., Barragan V., Supuran C.T. Carbonic anhydrase inhibitors: aliphatic N-phosphorylated sulfamates – A novel zinc-anchoring group leading to nanomolar inhibitors. Journal of Enzyme Inhibition and Medicinal Chemistry 2004, 19, 287-291.
26- Winum J-Y., Scozzafava A., Montero J-L., Supuran C.T. Therapeutic applications of sulfamates. Expert Opinion in Therapeutic Patents 2004, 14, 1273-1308.
25- Berredjem M., Winum J-Y., Toupet L., Aouf N-E, Montero J-L. N-ChlorosulfonylOxazolidin-2-ones: Synthesis, Structure and Reactivity toward Aminoesters. Synthetic Communications 2004, 34, 1653-1662.
24- Kadri M., Dhaoui N., Abdaoui M., Winum J-Y., Montero J-L. Inclusion Complexes of 2-Chloroethylnitrososulfamides (CENS) with b-Cyclodextrins. European Journal of Medicinal Chemistry 2004, 39, 79-84.
23- Bonnac L., Barragan V., Winum J-Y., Montero J-L. New pyrophosphate analogues: A facile access to N-(O-alkylsulfamoyl)phosphoramidic acids via a simple and quantitative reaction of N-(O-alkylsulfamate)trialkylphospha-λ5-azene with bromotrimethylsilane and water. Tetrahedron 2004, 60, 2187-2190.
22– Winum J-Y., Casini A., Mincione F., Starnotti M., Montero J-L., Scozzafava A., Supuran C.T. Carbonic anhydrase inhibitors: N-(p-sulfamoylphenyl)-b-D-glycopyranosylamines as topically acting antiglaucoma agents in hypertensive rabbits. Bioorganic and Medicinal Chemistry Letters 2004, 14, 225-229.
21– Abbate F., Winum J-Y., Potter B.V.L., Casini A., Montero J-L., Scozzafava A., Supuran Ct. Carbonic anhydrase inhibitors: X ray crystallographic structure of the adduct of human isozyme II with EMATE, a dual inhibitor of carbonic anhydrases and steroid sulfatases. Bioorganic and Medicinal Chemistry Letters 2004, 14, 231-234.
2003
20- Winum J-Y, Vullo D., Casini A., Montero J-L., Scozzafava A., Supuran C.T. Carbonic anhydrase inhibitors: Inhibition of transmembrane, tumor-associated isozyme IX and cytosolic isozymes I and II with aliphatic sulfamates. Journal of Medicinal Chemistry 2003, 46, 5471-5477.
19- Passagne I., Evrard A., Winum J-Y., Depeille P., Cuq P., Montero J-L., Cupissol D. Vian L. Cytotoxicity, DNA damage and apoptosis induced by new fotemustine analogues on human melanoma cells in relation to O6-methylguanine DNA-methyltransferase expression. Journal of Pharmacology and Experimental Therapeutics 2003, 307, 816-823.
18- Regainia Z., Winum J-Y., Smaine F-Z., Toupet L., Aouf N-E., Montero J-L. General Synthesis of n-Membered Cyclic Sulfamides. Tetrahedron 2003, 59, 6051-6056.
17- 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 the membrane-bound, tumor-associated isozyme IX with sulfamates also acting as steroid sulfatase inhibitors. Journal of Medicinal Chemistry 2003, 46, 2197-2204.
16- 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. Bioorganic and Medicinal Chemistry Letters 2003, 13, 837-840.
15- Winum J-Y., Bouissiere J-L., Passagne I., Evrard A., Montero V., Cuq P., Montero J-L. Synthesis and Biological Evaluation of Fotemustine Analogues on Human Melanoma Cell Lines. European Journal of Medicinal Chemistry 2003, 38, 319-324.
14- Berredjem M., Djebbar H., Regainia Z, Aouf N-E., Dewynter G., Winum J-Y., Montero J-L. Synthèse et N-Acylation Régiospécifique de 1,2,5-Thiadiazolidines 1,1-Dioxydes Chirales. Phosphorus, Sulfur and Silicon 2003, 178, 693-709.
2002
13- Winum J-Y., Commes T., Baghdiguian S., Leydet A., Montero J-L . Synthesis and Biological Activity of Targretin Analogs with Modified Polar Head. Bioorganic and Medicinal Chemistry Letters 2002, 12, 3529-3532.
2001
12- Winum J-Y., Toupet L., Barragan V., Dewynter G., Montero J-L. N-(tert-butoxycarbonyl)-N-[4-(dimethylazaniumylidene)-1,4-dihydropyridin-1-ylsulfonyl] azanide: A New Sulfamoylating Agent. Structure and Reactivity towards Amines. Organic Letters 2001, 3, 2241-2243.
11– Winum J-Y., Barragan V., Montero J-L Convenient Method for the Alkylation of Sulfamides using Alkyl Bromide and Mitsunobu Betaine. Tetrahedron Letters 2001, 42, 601-603.
10- Winum J-Y., Leydet A., Seman M., Montero J-L. Synthesis and Biological Activity of Glycosyl Conjugates of N-(4-Hydroxyphenyl retinamide). Il Farmaco 2001, 56, 319-324.
2000
9– Robert F., Winum J-Y., Sakai N., Gerard D., Matile S. Synthesis of Multiply Substituted Ion Channel Forming Octi(p-phenylene)s : Theme and Variations. Organic Letters 2000, 2, 37-39.
1999
8- Winum J-Y., Matile S. Rigid Push Pull Oligo(p-Phenylene) Rods: Depolarization of Bilayer Membranes with Negative Membrane Potential. Journal of American Chemical Society 1999, 121, 7961-7962.
7– Kamal M., Winum J-Y., Leydet A., Barragan V., Montero J-L. Synthesis and Biological Activity of a Retinyl Phosphonic Acid Derivative, an Analog of Retinyl Phosphate. Phosphorus, Sulfur and Silicon 1999, 152, 241-256.
1998
6– Sangmam C., Winum J-Y., Lucas M., Montero J-L., Chavis C. A simple, general and efficient method for O and N-retinoylation. Application to the synthesis of 2-retinoyl-lecithin. Synthetic Communications 1998, 28, 2945-2958.
5– Winum J-Y., Kamal M., Barragan V., Leydet A., Montero J-L. One pot synthesis of nucleosides using Bismuth III bromide as catalyst. Synthetic Communications 1998, 28, 603-606.
1997
4– Winum J-Y., Kamal M., Agnaniet H., Leydet A., Montero J-L. Etude de la réaction de Michaelis Arbuzov sous activation ultrasonore. Phosphorus, Sulfur and Silicon 1997, 129, 83-88.
3– Winum J-Y., Leydet A., Kamal M., Pavia A.A., Roque J-P, Montero J-L. A Convenient synthesis of peracetylated glycosyl halides using Bismuth (III) Halides as Catalysts. Carbohydrate Research 1997, 297, 175-180.
2– Winum J-Y., Kamal M., Defacque H., Commes T., Chavis C., Lucas M., Marti J., Montero J-L. Synthesis and Biological Activities of Higher Homologues of Retinoic Acid. Il Farmaco 1997, 52, 39-42.
1996
1- Winum J-Y., Kamal M., Leydet A., Roque J-P., Montero J-L. Homologation of Carboxylic Acids by Arndt-Eistert Reaction under Ultrasonic Waves. Tetrahedron Letters 1996, 37, 1781-1782.