O. Bruno

发表

New insights into selective PDE4D inhibitors: 3-(Cyclopentyloxy)-4-methoxybenzaldehyde O-(2-(2,6-dimethylmorpholino)-2-oxoethyl) oxime (GEBR-7b) structural development and promising activities to restore memory impairment.

L. Milanesi, E. Fedele, P. Fossa, 2016, European journal of medicinal chemistry.

A novel mechanism for cyclic adenosine monophosphate–mediated memory formation: Role of amyloid beta

E. Fedele, A. Palmeri, O. Arancio, 2014, Annals of neurology.

Synthesis, biological evaluation, and molecular modeling of new 3-(cyclopentyloxy)-4-methoxybenzaldehyde O-(2-(2,6-dimethylmorpholino)-2-oxoethyl) Oxime (GEBR-7b) related phosphodiesterase 4D (PDE4D) inhibitors.

E. Fedele, P. Fossa, C. Brullo, 2014, Journal of medicinal chemistry.

6-amino-4-oxo-1,3-diphenyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonyl derivatives as a new class of potent inhibitors of Interleukin-8-induced neutrophil chemotaxis.

M. Bertolotto, F. Dallegri, O. Bruno, 2009, Bioorganic & medicinal chemistry.

The pyrazolyl-urea GeGe3 inhibits tumor angiogenesis and reveals dystrophia myotonica protein kinase (DMPK)1 as a novel angiogenesis target

C. Brullo, Elda Meta, B. Imhof, 2017, Oncotarget.

Synthesis and 3D QSAR of new pyrazolo[3,4-b]pyridines: potent and selective inhibitors of A1 adenosine receptors.

M. Trincavelli, C. Martini, P. Fossa, 2005, Journal of medicinal chemistry.

Substituted Pyrazolo[3,4‐b]pyridines as Potent A1 Adenosine Antagonists: Synthesis, Biological Evaluation, and Development of an A1 Bovine Receptor Model

M. Trincavelli, C. Martini, C. Tintori, 2008, ChemMedChem.

3,5-Diphenyl-1H-pyrazole derivatives. IX. 2-substituted 4-phenyl-5-(3,5-diphenyl-1H-pyrazol-1-yl) pyrimidines with platelet antiaggregating and other activities.

P. Schenone, W. Filippelli, O. Bruno, 1992, Farmaco.

Synthesis and pharmacological evaluation of 5H-[1]benzopyrano[4,3-d]pyrimidines effective as antiplatelet/analgesic agents.

C. Brullo, S. Schenone, O. Bruno, 2004, Bioorganic & medicinal chemistry.

Synthesis and biological data of 4-amino-1-(2-chloro-2-phenylethyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid ethyl esters, a new series of A1-adenosine receptor (A1AR) ligands.

C. Martini, P. Fossa, S. Schenone, 2001, Bioorganic & medicinal chemistry letters.

Effects of subacute treatment with benzopyranopyrimidines in hemostasis and experimental thrombosis in mice.

O. Bruno, V. Ballabeni, E. Barocelli, 2004, Life sciences.

Synthesis, biological activities and pharmacokinetic properties of new fluorinated derivatives of selective PDE4D inhibitors.

E. Fedele, C. Brullo, R. Ricciarelli, 2015, Bioorganic & medicinal chemistry.

Pyrazolyl-Ureas as Interesting Scaffold in Medicinal Chemistry

C. Brullo, O. Bruno, Federica Rapetti, 2020, Molecules.

Synthesis, antiplatelet and antithrombotic activities of new 2-substituted benzopyrano[4,3-d]pyrimidin-4-cycloamines and 4-amino/cycloamino-benzopyrano[4,3-d]pyrimidin-5-ones.

C. Brullo, S. Schenone, M. Impicciatore, 2006, Bioorganic & medicinal chemistry.

Design, synthesis and biological evaluation of new pyrazolyl-ureas and imidazopyrazolecarboxamides able to interfere with MAPK and PI3K upstream signaling involved in the angiogenesis.

C. Brullo, Elda Meta, B. Imhof, 2017, European journal of medicinal chemistry.

Further Insights in the Binding Mode of Selective Inhibitors to Human PDE4D Enzyme Combining Docking and Molecular Dynamics

L. Milanesi, P. Fossa, E. Cichero, 2016, Molecular informatics.

2-Phenyl-2,3-dihydro-1H-imidazo[1,2-b]pyrazole derivatives: new potent inhibitors of fMLP-induced neutrophil chemotaxis.

C. Brullo, S. Schenone, M. Falzarano, 2007, Bioorganic & medicinal chemistry letters.

Synthesis and biological evaluation of neutrophilic inflammation inhibitors.

C. Brullo, S. Schenone, F. Dallegri, 2004, Farmaco.

Homology Modeling, Docking Studies and Molecular Dynamic Simulations Using Graphical Processing Unit Architecture to Probe the Type‐11 Phosphodiesterase Catalytic Site: A Computational Approach for the Rational Design of Selective Inhibitors

L. Milanesi, P. Fossa, E. Cichero, 2013, Chemical biology & drug design.

New 1,3,4-thiadiazole derivatives endowed with analgesic and anti-inflammatory activities.

C. Brullo, S. Schenone, W. Filippelli, 2006, Bioorganic & medicinal chemistry.

Selective PDE4 subtype inhibition provides new opportunities to intervene in neuroinflammatory versus myelin damaging hallmarks of multiple sclerosis

E. Fedele, K. Wasner, P. Wieringa, 2022, Brain, Behavior, and Immunity.

AN EFFICIENT SYNTHESIS OF FUNCTIONALIZED 2-PYRIDONES BY DIRECT ROUTE OR VIA AMIDE/ENOLATE AMMONIUM SALT INTERMEDIATES

O. Bruno, L. Mosti, G. Menozzi, 1999 .

N-arylsubstituted-1-aryl-3,4-diphenyl-5-pyrazole amines with analgesic and antiarrhythmic properties.

S. Schenone, W. Filippelli, O. Bruno, 1997, Farmaco.

Antiinflammatory agents: new series of N-substituted amino acids with complex pyrimidine structures endowed with antiphlogistic activity.

S. Schenone, W. Filippelli, F. Mazzeo, 1999, Farmaco.

Relative stereochemistry of a diterpene from Salvia cinnabarina.

B. Pagano, C. Mattia, A. Bisio, 2007, Molecules.

Synthesis and Pharmacological Evaluation of 2,5‐Cycloamino‐5H‐[1]benzopyrano[4,3‐d]pyrimidines Endowed with in vitro Antiplatelet Activity.

C. Brullo, S. Schenone, M. Chiavarini, 2001 .

3-Arylsulphonyl-5-arylamino-1,3,4-thiadiazol-2(3H)ones as anti-inflammatory and analgesic agents.

S. Schenone, W. Filippelli, O. Bruno, 2001, Bioorganic & medicinal chemistry.

Synthesis of new 5,6-dihydrobenzo[h]quinazoline 2,4-diamino substituted and antiplatelet/antiphlogistic activities evaluation.

P. Fossa, E. Cichero, C. Brullo, 2012, Bioorganic & medicinal chemistry letters.

Progress in 5H[1]benzopyrano[4,3-d]pyrimidin-5-amine series: 2-methoxy derivatives effective as antiplatelet agents with analgesic activity.

C. Brullo, S. Schenone, O. Bruno, 2002, Farmaco.

3-(Arylamino)-6,7-dihydro-6-methylpyrano[4,3-c]pyrazol-4(1H or 2H)-ones with antipyretic, analgesic, antiarrhythmic, hypotensive and other activities.

S. Schenone, L. Berrino, O. Bruno, 1993, Farmaco.

Identification of a novel pyrazolo[3,4-d]pyrimidine able to inhibit cell proliferation of a human osteogenic sarcoma in vitro and in a xenograft model in mice.

C. Brullo, G. Maga, S. Schenone, 2007, Journal of medicinal chemistry.

Synthesis and anti-inflammatory activity of esters derived from 5-aryl-1,2-dihydro-2-(2-hydroxyethyl)-3H-1,2,4-triazole-3-thiones.

S. Schenone, W. Filippelli, O. Bruno, 1998, Farmaco.

Synthesis and pharmacological evaluation of 2,5-cycloamino-5H-[1]benzopyrano[4,3-d]pyrimidines endowed with in vitro antiplatelet activity.

C. Brullo, S. Schenone, M. Chiavarini, 2001, Bioorganic & medicinal chemistry letters.

Preparation of new 5-aroylamino substituted 3-nicotinoyl/isonicotinoyl-1,3,4-thiadiazol-2(3H)-ones with anti-inflammatory activity.

S. Schenone, W. Filippelli, O. Bruno, 1998, Farmaco.

4-Amino-Substituted Pyrazolo[3,4-d]Pyrimidines: Synthesis and Biological Properties

M. Radi, S. Schenone, M. Botta, 2009 .

Structure-based optimization of pyrazolo[3,4-d]pyrimidines as Abl inhibitors and antiproliferative agents toward human leukemia cell lines.

M. Trincavelli, C. Martini, C. Brullo, 2008, Journal of medicinal chemistry.

Synthesis and biological evaluation of N-pyrazolyl-N'-alkyl/benzyl/phenylureas: a new class of potent inhibitors of interleukin 8-induced neutrophil chemotaxis.

Fabrizio Montecucco, Silvia Schenone, Massimiliano Tognolini, 2007, Journal of medicinal chemistry.

New pyrazolo[3,4-d]pyrimidines endowed with A431 antiproliferative activity and inhibitory properties of Src phosphorylation.

P. Fossa, C. Brullo, S. Schenone, 2004, Bioorganic & medicinal chemistry letters.

3,5-diphenyl-1H-pyrazole derivatives. XI. N-aryl-5(3)-phenyl-4-(3,5- diphenyl-1-pyrazolyl)-3(5)-pyrazole amines, 5-substituted 4,5-dihydro-3-phenyl-4-(3,5-diphenyl-1-pyrazolyl)-1H-pyrazoles and 2,6-disubstituted 1,6-dihydro-4- phenyl-5-(3,5-diphenyl-1-pyrazolyl)pyrimidines with antipyretic, antiinfl

P. Schenone, W. Filippelli, A. Filippelli, 1993, Farmaco.

Synthesis and antiproliferative activity of basic thioanalogues of merbarone.

S. Schenone, R. Loddo, P. la Colla, 2003, Bioorganic & medicinal chemistry.

2-Amino/azido/hydrazino-5-alkoxy-5H-[1]benzopyrano[4,3-d]pyrimidines: synthesis and pharmacological evaluation.

C. Brullo, S. Schenone, O. Bruno, 2007, Medicinal chemistry (Shariqah (United Arab Emirates)).

2-aryl-3-phenylamino-4,5-dihydro-2h-benz[g]indazoles with analgesic activity.

C. Brullo, S. Schenone, W. Filippelli, 2003, Farmaco.

New polycyclic pyrimidine derivatives with antiplatelet in vitro activity: synthesis and pharmacological screening.

S. Schenone, M. Chiavarini, M. Impicciatore, 2001, Bioorganic & medicinal chemistry.

N-substituted 3-(arylamino)-4,5-dihydro-2H-benz[g]indazol-2-yl acetamides with anti-inflammatory and analgesic activities.

S. Schenone, W. Filippelli, O. Bruno, 2000, Farmaco.

Pyrazolo[3,4-d]pyrimidines as potent antiproliferative and proapoptotic agents toward A431 and 8701-BC cells in culture via inhibition of c-Src phosphorylation.

M. Modugno, P. Fossa, C. Tintori, 2006, Journal of medicinal chemistry.

Docking-based CoMFA and CoMSIA analyses of tetrahydro-β-carboline derivatives as type-5 phosphodiesterase inhibitors

P. Fossa, E. Cichero, O. Bruno, 2012, Journal of enzyme inhibition and medicinal chemistry.

1-Methyl and 1-(2-hydroxyalkyl)-5-(3-alkyl/cycloalkyl/phenyl/naphthylureido)-1H-pyrazole-4-carboxylic acid ethyl esters as potent human neutrophil chemotaxis inhibitors.

C. Brullo, S. Schenone, M. Falzarano, 2009, Bioorganic & medicinal chemistry.

Synthesis of N-substituted-N-acylthioureas of 4-substituted piperazines endowed with local anaesthetic, antihyperlipidemic, antiproliferative activities and antiarrythmic, analgesic, antiaggregating actions.

P. Fossa, S. Schenone, W. Filippelli, 2003, Farmaco.

Differential inhibition of signaling pathways by two new imidazo-pyrazoles molecules in fMLF-OMe- and IL8-stimulated human neutrophil.

C. Brullo, O. Bruno, R. Selvatici, 2013, European journal of pharmacology.

N-Aryl-2-phenyl-2,3-dihydro-imidazo[1,2-b]pyrazole-1-carboxamides 7-substituted strongly inhibiting both fMLP-OMe- and IL-8-induced human neutrophil chemotaxis.

C. Brullo, O. Bruno, R. Selvatici, 2012, European journal of medicinal chemistry.

1-Acyl-, 3-acyl- and 1,3-diacyl-3-furfuryl-1-phenylthioureas with platelet antiaggregating and other activities.

S. Schenone, O. Bruno, F. Rossi, 1991, Farmaco.

Antiproliferative activity of new 1-aryl-4-amino-1H-pyrazolo[3,4-d]pyrimidine derivatives toward the human epidermoid carcinoma A431 cell line.

P. Fossa, S. Schenone, M. Botta, 2004, European journal of medicinal chemistry.

O-[2-hydroxy-3-(dialkylamino)propyl]ethers of (+)-1,7,7-trimethyl bicyclo[2.2.1]heptan-2-one oxime (camphor oxime) with analgesic and antiarrhythmic activities.

S. Schenone, W. Filippelli, O. Bruno, 2000, Farmaco.

Pyrazole and imidazo[1,2-b]pyrazole Derivatives as New Potential Antituberculosis Agents.

C. Brullo, Elda Meta, S. Franzblau, 2019, Medicinal chemistry (Shariqah (United Arab Emirates)).

New Series of Pyrazoles and Imidazo-Pyrazoles Targeting Different Cancer and Inflammation Pathways

C. Brullo, Elda Meta, O. Bruno, 2021, Molecules.

Synthesis, molecular modeling studies, and pharmacological activity of selective A(1) receptor antagonists.

C. Martini, P. Fossa, S. Schenone, 2002, Journal of medicinal chemistry.

Parallel one-pot synthesis and structure-activity relationship study of symmetric formimidoester disulfides as a novel class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.

S. Schenone, R. Loddo, G. Sanna, 2008, Bioorganic & medicinal chemistry.

Biological evaluation of pyrazolyl-urea and dihydro-imidazo-pyrazolyl-urea derivatives as potential anti-angiogenetic agents in the treatment of neuroblastoma

C. Brullo, Elda Meta, B. Marengo, 2020, Oncotarget.

Novel modifications in the series of O-(2-phthalimidoethyl)-N-substituted thiocarbamates and their ring-opened congeners as non-nucleoside HIV-1 reverse transcriptase inhibitors.

S. Schenone, R. Loddo, G. Sanna, 2009, European journal of medicinal chemistry.

New insights into small‐molecule inhibitors of Bcr‐Abl

M. Radi, S. Schenone, M. Botta, 2011, Medicinal research reviews.

Synthesis, functional proteomics and biological evaluation of new 5-pyrazolyl ureas as potential anti-angiogenic compounds.

C. Brullo, M. Monti, Elda Meta, 2021, European journal of medicinal chemistry.

New Hybrid Pyrazole and Imidazopyrazole Antinflammatory Agents Able to Reduce ROS Production in Different Biological Targets

C. Brullo, F. Montecucco, S. Alfei, 2020, Molecules.

Synthesis and Pharmacological Screening of Novel Non-acidic Gastroprotective Antipyretic Anti-inflammatory Agents with Anti-platelet Properties

S. Schenone, M. Chiavarini, O. Bruno, 2000, Arzneimittelforschung.

Synthesis, biological evaluation and docking studies of 4-amino substituted 1H-pyrazolo[3,4-d]pyrimidines.

C. Tintori, C. Brullo, E. Crespan, 2008, European journal of medicinal chemistry.

3,5-Diphenyl-1H-pyrazole derivatives. XII. N-substituted 4-amino-1-(2-hydroxy- or 2-alkylaminoethyl)-3,5-diphenyl-1H-pyrazoles with local anesthetic, analgesic and platelet antiaggregating activities.

S. Schenone, A. Filippelli, O. Bruno, 1994, Farmaco.

Structure-based design, parallel synthesis, structure-activity relationship, and molecular modeling studies of thiocarbamates, new potent non-nucleoside HIV-1 reverse transcriptase inhibitor isosteres of phenethylthiazolylthiourea derivatives.

Silvia Schenone, Alessandra Pani, Paola Fossa, 2005, Journal of medicinal chemistry.

Memory-enhancing effects of GEBR-32a, a new PDE4D inhibitor holding promise for the treatment of Alzheimer’s disease

Elentina K. Argyrousi, E. Fedele, O. Arancio, 2017, Scientific Reports.

Selective PDE4 subtype inhibition provides new opportunities to intervene in neuroinflammatory versus myelin damaging hallmarks of multiple sclerosis

E. Fedele, K. Wasner, P. Wieringa, 2022, Brain, Behavior, and Immunity.

GEBR‐7b, a novel PDE4D selective inhibitor that improves memory in rodents at non‐emetic doses

E. Fedele, C. Brullo, E. Gardella, 2011, British journal of pharmacology.

New insights into PDE4B inhibitor selectivity: CoMFA analyses and molecular docking studies

P. Fossa, E. Cichero, Sara Guariento, 2016, Molecular Diversity.

PDE4D inhibitors: A potential strategy for the treatment of memory impairment?

E. Fedele, J. Prickaerts, L. Parker, 2014, Neuropharmacology.

Synthesis of 1-(2-chloro-2-phenylethyl)-6-methylthio-1H-pyrazolo[3,4-d]pyrimidines 4-amino substituted and their biological evaluation.

C. Martini, P. Fossa, S. Schenone, 2004, European journal of medicinal chemistry.

The Pyrazolyl-Urea Gege3 Inhibits the Activity of ANXA1 in the Angiogenesis Induced by the Pancreatic Cancer Derived EVs

C. Brullo, A. Petrella, O. Bruno, 2021, Biomolecules.

Design, synthesis, SAR, and molecular modeling studies of acylthiocarbamates: a novel series of potent non-nucleoside HIV-1 reverse transcriptase inhibitors structurally related to phenethylthiazolylthiourea derivatives.

S. Schenone, P. la Colla, A. Pani, 2003, Journal of medicinal chemistry.

Parallel synthesis, molecular modelling and further structure-activity relationship studies of new acylthiocarbamates as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.

S. Schenone, M. Pezzullo, R. Loddo, 2009, European journal of medicinal chemistry.

Thiocarbamates as non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 2: Parallel synthesis, molecular modelling and structure-activity relationship studies on analogues of O-(2-phenylethyl)-N-phenylthiocarbamate.

R. Loddo, P. la Colla, O. Bruno, 2008, Bioorganic & medicinal chemistry.

Design, synthesis, biological evaluation and structural characterization of novel GEBR library PDE4D inhibitors.

C. Brullo, Tommaso Prosdocimi, E. Parisini, 2021, European journal of medicinal chemistry.

Insight into GEBR-32a: Chiral Resolution, Absolute Configuration and Enantiopreference in PDE4D Inhibition

C. Brullo, F. Vasile, E. Parisini, 2020, Molecules.

New selective phosphodiesterase 4D inhibitors differently acting on long, short, and supershort isoforms.

C. Brullo, S. Schenone, Alessia Romussi, 2009, Journal of medicinal chemistry.

A1 Receptors Ligands: Past, Present and Future Trends

F. Musumeci, C. Brullo, S. Schenone, 2010 .

N-Acyl-N-phenyl ureas of piperidine and substituted piperidines endowed with anti-inflammatory and anti-proliferative activities.

S. Schenone, W. Filippelli, O. Bruno, 2001, Farmaco.

Exhaustive 3D-QSAR analyses as a computational tool to explore the potency and selectivity profiles of thieno[3,2-d]pyrimidin-4(3H)-one derivatives as PDE7 inhibitors

P. Fossa, E. Cichero, C. Brullo, 2016 .

Synthesis and biological evaluation of [alpha-(1,5-disubstituted 1H-pyrazol-4-yl)benzyl]azoles, analogues of bifonazole.

W. Filippelli, P. la Colla, O. Bruno, 1999, Farmaco.

3D QSAR Models Built on Structure‐Based Alignments of Abl Tyrosine Kinase Inhibitors

Fabrizio Manetti, Maurizio Botta, Silvia Schenone, 2009, ChemMedChem.

Pyrazolo[3,4-d]pyrimidines endowed with antiproliferative activity on ductal infiltrating carcinoma cells.

P. Fossa, C. Brullo, S. Schenone, 2004, Journal of medicinal chemistry.

Phosphodiesterase isoform‐specific expression induced by traumatic brain injury

C. Atkins, A. Oliva, O. Alonso, 2012, Journal of neurochemistry.

Improvement of spatial memory function in APPswe/PS1dE9 mice after chronic inhibition of phosphodiesterase type 4D

E. Fedele, A. Sierksma, J. Prickaerts, 2014, Neuropharmacology.

Substituted Pyrazolo[3,4‐b]pyridines as Potent A1 Adenosine Antagonists: Synthesis, Biological Evaluation, and Development of an A1 Bovine Receptor Model

M. Trincavelli, C. Martini, C. Tintori, 2008, ChemMedChem.

Design and synthesis of 4,5,6,7-tetrahydro-1H-1,2-diazepin-7-one derivatives as a new series of Phosphodiesterase 4 (PDE4) inhibitors.

P. Fossa, F. Giordanetto, Sara Guariento, 2017, Bioorganic & medicinal chemistry letters.

The pyrazolyl-urea GeGe3 inhibits tumor angiogenesis and reveals dystrophia myotonica protein kinase (DMPK)1 as a novel angiogenesis target

C. Brullo, Elda Meta, B. Imhof, 2017, Oncotarget.

Docking-based CoMFA and CoMSIA analyses of tetrahydro-β-carboline derivatives as type-5 phosphodiesterase inhibitors

P. Fossa, E. Cichero, O. Bruno, 2012, Journal of enzyme inhibition and medicinal chemistry.

Benzimidazole-based derivatives as privileged scaffold developed for the treatment of the RSV infection: a computational study exploring the potency and cytotoxicity profiles

P. Fossa, E. Cichero, R. Loddo, 2017, Journal of enzyme inhibition and medicinal chemistry.