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Author Silvia Selleri

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Privileged scaffolds in medicinal chemistry: Studies on pyrazolo[1,5-a]pyrimidines on sulfonamide containing Carbonic Anhydrase inhibitors.

Arzu Gumus, Murat Bozdag, Andrea Angeli, Thomas S Peat, Fabrizio Carta, Claudiu T Supuran, Silvia Selleri,

We report for the first time a small series of compounds endowed in vitro with inhibitory properties for the human (h) expressed Carbonic Anhydrase (CAs, E.C. 4.2.1.1) enzymes of physiological interest (i.e. I, II, VA, IX and XII) and bearing the pyrazolo[1,5-a]pyrimidine (PP) scaffold at the tail section. Among the ... Read more >>

Bioorg Med Chem Lett (Bioorganic & medicinal chemistry letters)
[2021, 49:128309]

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Structural Insights into Schistosoma mansoni Carbonic Anhydrase (SmCA) Inhibition by Selenoureido-Substituted Benzenesulfonamides.

Andrea Angeli, Marta Ferraroni, Akram A Da'dara, Silvia Selleri, Mariana Pinteala, Fabrizio Carta, Patrick J Skelly, Claudiu T Supuran,

Tegumental carbonic anhydrase from the worm <i>Schistosoma mansoni</i> (SmCA) is considered a new anti-parasitic target because suppressing its expression interferes with schistosome metabolism and virulence. Here, we present the inhibition profiles of selenoureido compounds on recombinant SmCA and resolution of the first X-ray crystal structures of SmCA in adduct with ... Read more >>

J Med Chem (Journal of medicinal chemistry)
[2021, 64(14):10418-10428]

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Tellurides bearing benzensulfonamide as carbonic anhydrase inhibitors with potent antitumor activity.

Andrea Angeli, Mariana Pinteala, Stelian S Maier, Alessandra Toti, Lorenzo Di Cesare Mannelli, Carla Ghelardini, Silvia Selleri, Fabrizio Carta, Claudiu T Supuran,

We evaluated in vitro a series of telluride containing compounds bearing the benzenesulfonamide group, as effective inhibitors of the physiologically relevant human (h) expressed Carbonic Anhydrase (CA; EC 4.2.1.1) enzymes I, II, IV VII and IX. The potent effects of such compounds against the tumor-associated hCA IX being low nanomolar ... Read more >>

Bioorg Med Chem Lett (Bioorganic & medicinal chemistry letters)
[2021, 45:128147]

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Taurultams incorporating arylsulfonamide: First in vitro inhibition studies of α-, β- and γ-class Carbonic Anhydrases from Vibrio cholerae and Burkholderia pseudomallei.

Ozlem Akgul, Andrea Angeli, Silvia Selleri, Clemente Capasso, Claudiu T Supuran, Fabrizio Carta,

A new series of taurultambenzenesulfonamides 1-17 were prepared and considered for their inhibitory activity in vitro against the Carbonic Anhydrases from Vibrio cholerae (VchCA-α, VchCA-β and VchCA-γ) and Burkholderia pseudomallei (BpsCA-β and BpsCA-γ). Among the compounds tested, derivatives 4, 5, 7, 10, 12, and 16 resulted in highly effective VchCAα inhibitors ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2021, 219:113444]

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Polypharmacology of epacadostat: a potent and selective inhibitor of the tumor associated carbonic anhydrases IX and XII.

Andrea Angeli, Marta Ferraroni, Alessio Nocentini, Silvia Selleri, Paola Gratteri, Claudiu T Supuran, Fabrizio Carta,

Epacadostat (EPA), a selective indoleamine-2,3-dioxygenase 1 (IDO1) inhibitor, has been investigated in vitro as a human (h) Carbonic Anhydrase Inhibitor (CAI). The kinetic data clearly show, for the first time, EPA to be a highly effective and selective inhibitor for the tumor-associated isoforms hCA IX/XII. We report the high resolution ... Read more >>

Chem Commun (Camb) (Chemical communications (Cambridge, England))
[2019, 55(40):5720-5723]

Cited: 1 time

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Handling drug-target selectivity: A study on ureido containing Carbonic Anhydrase inhibitors.

Ozlem Akgul, Srishti Singh, Jacob T Andring, Robert McKenna, Silvia Selleri, Fabrizio Carta, Andrea Angeli, Claudiu T Supuran,

Here we report the synthesis of a series of taurine substituted sulfonamide derivatives 1-29 having the ureido moiety installed at the tail section as selective inhibitors of the tumor associated human (h) Carbonic Anhydrase (CA; EC 4.2.1.1) IX and XII. The series was deeply investigated for their kinetic features which ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2021, 212:113035]

Cited: 1 time

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Leveraging complex interactions between signaling pathways involved in liver development to robustly improve the maturity and yield of pluripotent stem cell-derived hepatocytes

Claudia Raggi, Marie-Agnès M’Callum, Quang Toan Pham, Perrine Gaub, Silvia Selleri, Nissan Baratang, Chenicka Lyn Mangahas, Gaël Cagnone, Bruno Reversade, Jean-Sébastien Joyal, Massimiliano Paganelli,

<h4>SUMMARY</h4> Pluripotent stem cell (PSC)-derived hepatocyte-like cells (HLC) have shown great potential as an alternative to primary human hepatocytes (PHH) for in vitro modeling. Several differentiation protocols have been described to direct PSC towards the hepatic fate, although the resulting HLC have shown more a fetal than adult phenotype. Here, ... Read more >>

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Azidothymidine "Clicked" into 1,2,3-Triazoles: First Report on Carbonic Anhydrase-Telomerase Dual-Hybrid Inhibitors.

Emanuela Berrino, Andrea Angeli, Dmitry D Zhdanov, Anna P Kiryukhina, Andrea Milaneschi, Alessandro De Luca, Murat Bozdag, Simone Carradori, Silvia Selleri, Gianluca Bartolucci, Thomas S Peat, Marta Ferraroni, Claudiu T Supuran, Fabrizio Carta,

Cancer cells rely on the enzyme telomerase (EC 2.7.7.49) to promote cellular immortality. Telomerase inhibitors (i.e., azidothymidine) can represent promising antitumor agents, although showing high toxicity when administered alone. Better outcomes were observed within a multipharmacological approach instead. In this context, we exploited the validated antitumor targets carbonic anhydrases (CAs; ... Read more >>

J Med Chem (Journal of medicinal chemistry)
[2020, 63(13):7392-7409]

Cited: 2 times

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X-ray crystallography of Epacadostat in adduct with Carbonic Anhydrase IX.

Andrea Angeli, Thomas S Peat, Silvia Selleri, Abdulmalik Saleh Alfawaz Altamimi, Claudiu T Supuran, Fabrizio Carta,

Epacadostat (EPA), a new and promising anti-cancer small molecule is firmly established as selective inhibitor of the enzyme indoleamine 2,3-dioxygenase 1 (IDO1). The X-Ray structure of the human CA IX mimic in complex with EPA is investigated here for the first time and compared to previously reported EPA-CA II adduct. ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2020, 97:103669]

Cited: 1 time

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Bioisosteric Development of Multitarget Nonsteroidal Anti-Inflammatory Drug-Carbonic Anhydrases Inhibitor Hybrids for the Management of Rheumatoid Arthritis.

Silvia Bua, Laura Lucarini, Laura Micheli, Marta Menicatti, Gianluca Bartolucci, Silvia Selleri, Lorenzo Di Cesare Mannelli, Carla Ghelardini, Emanuela Masini, Fabrizio Carta, Paola Gratteri, Alessio Nocentini, Claudiu T Supuran,

Multitarget nonsteroidal anti-inflammatory drug (NSAID)-carbonic anhydrase inhibitor (CAI) agents for the management of rheumatoid arthritis are reported. The evidence of the plasma stability of the amide-linked hybrids previously reported prompted us to investigate their pain-relieving mechanism of action. A bioisosteric amide to ester substitution yielded a series of derivatives showing ... Read more >>

J Med Chem (Journal of medicinal chemistry)
[2020, 63(5):2325-2342]

Cited: 6 times

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Efficient and Robust NK-Cell Transduction With Baboon Envelope Pseudotyped Lentivector.

Aurelien B L Colamartino, William Lemieux, Panojot Bifsha, Simon Nicoletti, Nitin Chakravarti, Joaquín Sanz, Hugo Roméro, Silvia Selleri, Kathie Béland, Mélanie Guiot, Camille Tremblay-Laganière, Renée Dicaire, Luis Barreiro, Dean A Lee, Els Verhoeyen, Elie Haddad,

NK-cell resistance to transduction is a major technical hurdle for developing NK-cell immunotherapy. By using Baboon envelope pseudotyped lentiviral vectors (BaEV-LVs) encoding eGFP, we obtained a transduction rate of 23.0 ± 6.6% (mean ± SD) in freshly-isolated human NK-cells (FI-NK) and 83.4 ± 10.1% (mean ± SD) in NK-cells obtained ... Read more >>

Front Immunol (Frontiers in immunology)
[2019, 10:2873]

Cited: 20 times

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N-aryl-N'-ureido-O-sulfamates: Potent and selective inhibitors of the human Carbonic Anhydrase VII isoform with neuropathic pain relieving properties.

Murat Bozdag, Giulio Poli, Andrea Angeli, Elena Lucarini, Tiziano Tuccinardi, Lorenzo Di Cesare Mannelli, Silvia Selleri, Carla Ghelardini, Jean-Yves Winum, Fabrizio Carta, Claudiu T Supuran,

Herein we report for the first time an efficient synthetic procedure for the preparation of N-aryl-N'-ureido-O-sulfamates (AUSs) as a new class of Carbonic Anhydrase Inhibitors (CAIs). The compounds were tested for the inhibition of several human (h) Carbonic Anhydrase (CA; EC 4.2.1.1) isoforms. Interesting inhibition activity and high selectivity against ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2019, 89:103033]

Cited: 3 times

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β3-Adrenoreceptor Activity Limits Apigenin Efficacy in Ewing Sarcoma Cells: A Dual Approach to Prevent Cell Survival.

Amada Pasha, Marina Vignoli, Angela Subbiani, Alessio Nocentini, Silvia Selleri, Paola Gratteri, Annalisa Dabraio, Tommaso Casini, Luca Filippi, Ilaria Fotzi, Claudio Favre, Maura Calvani,

Ewing Sarcoma (ES) is an aggressive paediatric tumour where oxidative stress and antioxidants play a central role in cancer therapy response. Inhibiting antioxidants expression, while at the same time elevating intracellular reactive oxygen species (ROS) levels, have been proposed as a valid strategy to overcome ES cancer progression. Flavonoid intake ... Read more >>

Int J Mol Sci (International journal of molecular sciences)
[2019, 20(9):]

Cited: 2 times

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Efficient and robust NK-Cell transduction with Baboon Envelope pseudotyped lentivector: a major tool for immunotherapy

Aurelien B.L. Colamartino, William Lemieux, Panojot Bifsha, Simon Nicoletti, Nitin Chakravarti, Joaquin Sanz Remon, Hugo Roméro, Silvia Selleri, Kathie Béland, Mélanie Guiot, Camille Tremblay-Laganière, Renée Dicaire, Luis Barreiro, Dean Lee, Els Verhoeyen, Elie Haddad,

<h4>ABSTRACT</h4> NK-cell resistance to transduction is a major technical hurdle for developing NK-cell immunotherapy. By using Baboon envelope pseudotyped lentiviral vectors (BaEV-LVs) encoding eGFP, we obtained a transduction rate of 23.0±6.6% in freshly-isolated NK-cells (FI-NK) and 83.4±10.1% in NK-cells obtained from the NK-cell Activation and Expansion System (NKAES), even at ... Read more >>

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Discovery of new organoselenium compounds as antileishmanial agents.

Abdul-Malek S Al-Tamimi, Mikel Etxebeste-Mitxeltorena, Carmen Sanmartín, Antonio Jiménez-Ruiz, Leo Syrjänen, Seppo Parkkila, Silvia Selleri, Fabrizio Carta, Andrea Angeli, Claudiu T Supuran,

We report new organoselenium compounds bearing the sulfonamide moiety as effective inhibitors of the β-isoform of Carbonic Anhydrase from the unicellular parasitic protozoan L. donovani chagasi. All derivatives were evaluated in vitro for their leishmanicidal activities against Leishmania infantum amastigotes along with their cytotoxicities in human THP-1 cells. Compounds 3e-g ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2019, 86:339-345]

Cited: 1 time

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N-Nitrosulfonamides as Carbonic Anhydrase Inhibitors: A Promising Chemotype for Targeting Chagas Disease and Leishmaniasis.

Alessandro Bonardi, Alane Beatriz Vermelho, Veronica da Silva Cardoso, Mirian Claudia de Souza Pereira, Leonardo da Silva Lara, Silvia Selleri, Paola Gratteri, Claudiu T Supuran, Alessio Nocentini,

<i>Trypanosoma cruzi</i> and Leishmania spp. are protozoa of the Trypanosomatidae family, respectively, responsible of the neglected tropical disorders (NTDs) Chagas disease and leishmaniasis. The present pharmacotherapy is often ineffective and exhibits serious side effects. The metalloenzyme carbonic anhydrases (CAs, EC 4.2.1.1) recently identified in these protozoans (α-TcCA and β-LdcCA) are ... Read more >>

ACS Med Chem Lett (ACS medicinal chemistry letters)
[2019, 10(4):413-418]

Cited: 3 times

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Carbonic Anhydrase Inhibitors of Different Structures Dilate Pre-Contracted Porcine Retinal Arteries.

Thor Eysteinsson, Hrönn Gudmundsdottir, Arnar Oessur Hardarson, Emanuela Berrino, Silvia Selleri, Claudiu T Supuran, Fabrizio Carta,

Carbonic anhydrase inhibitors (CAIs), such as dorzolamide (DZA), are used as anti-glaucoma drugs to lower intraocular pressure, but it has been found that some of these drugs act as vasodilators of retinal arteries. The exact mechanism behind the vasodilatory effect is not yet clear. Here we have addressed the issue ... Read more >>

Int J Mol Sci (International journal of molecular sciences)
[2019, 20(3):]

Cited: 2 times

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Rapamycin as an Adjunctive Therapy for NLRC4 Associated Macrophage Activation Syndrome.

Julie Barsalou, Annaliesse Blincoe, Isabel Fernandez, Dorothée Dal-Soglio, Lorie Marchitto, Silvia Selleri, Elie Haddad, Aissa Benyoucef, Fabien Touzot,

Gain of function (GOF) mutations affecting the inflammasome component NLRC4 are known to cause early-onset macrophage activation syndrome (MAS) and neonatal enterocolitis. Here we report a patient with a NLRC4 GOF mutation presenting with neonatal MAS efficiently treated with a combination of anakinra and rapamycin. Through <i>in vitro</i> studies, we ... Read more >>

Front Immunol (Frontiers in immunology)
[2018, 9:2162]

Cited: 7 times

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Remarkable Enhancement in Boron Uptake Within Glioblastoma Cells With Carboranyl-Indole Carboxamides.

Rajeshwar Narlawar, Christopher J D Austin, Jan Kahlert, Silvia Selleri, Eleonora Da Pozzo, Claudia Martini, Eryn L Werry, Louis M Rendina, Michael Kassiou,

Novel boron-rich, carboranyl-indole carboxamide ligands were prepared and found to effectively target the 18 kDa translocator protein (TSPO), an upregulated mitochondrial membrane-bound protein which has been observed in variety of tumor cell lines and its expression appears to be proportional to the degree of tumorigenicity, emphasizing a key role in cancer ... Read more >>

Chem Asian J (Chemistry, an Asian journal)
[2018, 13(21):3321-3327]

Cited: 0 times

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Deciphering the Mechanism of Human Carbonic Anhydrases Inhibition with Sulfocoumarins: Computational and Experimental Studies.

Alessio Nocentini, Fabrizio Carta, Muhammet Tanc, Silvia Selleri, Claudiu T Supuran, Carla Bazzicalupi, Paola Gratteri,

The reaction mechanism of the carbonic anhydrase-mediated hydrolysis of sulfocoumarins to sulfonic acids has been investigated on an enzyme cluster model using the B3LYP hybrid density functional theory (DFT) and the QST procedure for the Transition State (TS) search. A multistep process was highlighted, with the rate-determining step identified in ... Read more >>

Chemistry (Chemistry (Weinheim an der Bergstrasse, Germany))
[2018, 24(31):7840-7844]

Cited: 9 times

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A new class of pyrazolo[5,1-c][1,2,4]triazines as γ-aminobutyric type A (GABAA) receptor subtype ligand: synthesis and pharmacological evaluation.

Gabriella Guerrini, Giovanna Ciciani, Simona Daniele, Claudia Martini, Camilla Costagli, Chiara Guarino, Silvia Selleri,

A comparison between compounds with pyrazolo[1,5-a]pyrimidine structure (series 4-6) and pyrazolo[5,1-c][1,2,4]triazine core (series 9) as ligands at GABAA-receptor subtype, was evaluated. Moreover, for pyrazolotriazine derivatives having binding recognition, the interaction on recombinant rat α(1-3,5) GABAA receptor subtypes, was performed. Among these latter, emerge compounds 9c, 9k, 9l, 9m and 9n ... Read more >>

Bioorg Med Chem (Bioorganic & medicinal chemistry)
[2018, 26(9):2475-2487]

Cited: 2 times

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Discovery of β-Adrenergic Receptors Blocker-Carbonic Anhydrase Inhibitor Hybrids for Multitargeted Antiglaucoma Therapy.

Alessio Nocentini, Mariangela Ceruso, Silvia Bua, Carrie L Lomelino, Jacob T Andring, Robert McKenna, Cecilia Lanzi, Silvia Sgambellone, Riccardo Pecori, Rosanna Matucci, Luca Filippi, Paola Gratteri, Fabrizio Carta, Emanuela Masini, Silvia Selleri, Claudiu T Supuran,

The combination of a β-adrenergic receptors (AR) blocker and a carbonic anhydrase (CA, EC 4.2.1.1) inhibitor in eye drops formulations is one of the most clinically used treatment for glaucoma. A novel approach consisting of single-molecule, multitargeted compounds for the treatment of glaucoma is proposed here by designing compounds which ... Read more >>

J Med Chem (Journal of medicinal chemistry)
[2018, 61(12):5380-5394]

Cited: 6 times

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Synthesis and pharmacological evaluation of pyrazolo[1,5-a]pyrimidin-7(4H)-one derivatives as potential GABAA-R ligands.

Gabriella Guerrini, Giovanna Ciciani, Simona Daniele, Lorenzo Di Cesare Mannelli, Carla Ghelardini, Claudia Martini, Silvia Selleri,

The synthesis of a new series of 6-phenyl- and 6-benzylpyrazolo[1,5-a]pyrimidin-7(4H)-ones 2a-g and 3a-g, strictly related to derivatives with pyrazolobenzotriazine (PBT) and pyrazoloquinazoline (PQ) scaffold, was realized. The in vitro GABA<sub>A</sub>-receptor subtype affinity was evaluated and from preliminary pharmacological studies, compound 3g shows anxiolytic-like effect at 10-30mg/kg. ... Read more >>

Bioorg Med Chem (Bioorganic & medicinal chemistry)
[2017, 25(6):1901-1906]

Cited: 2 times

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Human mesenchymal stromal cell-secreted lactate induces M2-macrophage differentiation by metabolic reprogramming.

Silvia Selleri, Panojot Bifsha, Sara Civini, Consiglia Pacelli, Mame Massar Dieng, William Lemieux, Ping Jin, Renée Bazin, Natacha Patey, Francesco M Marincola, Florina Moldovan, Charlotte Zaouter, Louis-Eric Trudeau, Basma Benabdhalla, Isabelle Louis, Christian Beauséjour, David Stroncek, Françoise Le Deist, Elie Haddad,

Human mesenchymal stromal cells (MSC) have been shown to dampen immune response and promote tissue repair, but the underlying mechanisms are still under investigation. Herein, we demonstrate that umbilical cord-derived MSC (UC-MSC) alter the phenotype and function of monocyte-derived dendritic cells (DC) through lactate-mediated metabolic reprogramming. UC-MSC can secrete large ... Read more >>

Oncotarget (Oncotarget)
[2016, 7(21):30193-30210]

Cited: 45 times

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Role of Natural Killer Cells in Intravenous Immunoglobulin-Induced Graft-versus-Host Disease Inhibition in NOD/LtSz-scidIL2rg(-/-) (NSG) Mice.

Joëlle Gregoire-Gauthier, François Fontaine, Lionel Benchimol, Simon Nicoletti, Silvia Selleri, Mame Massar Dieng, Elie Haddad,

Although clinical studies have yet to demonstrate clearly the use of intravenous immunoglobulin (IVIG) for prevention of graft-versus-host disease (GVHD), their effective use in a xenogeneic mouse model has been demonstrated. We aimed to determine the mechanism of action by which IVIG contributes to GVHD prevention in a xenogeneic mouse ... Read more >>

Biol Blood Marrow Transplant (Biology of blood and marrow transplantation : journal of the American Society for Blood and Marrow Transplantation)
[2015, 21(5):821-828]

Cited: 7 times

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