NMS Company
Pubblicazioni
Pubblicazioni
2008
Successful treatment of Imatinib resistant chronic myeloid leukemia cell lines and primary CD34+ cells by a small molecule inhibitor PHA-739358 is mediated by inhibition of both – Bcr-Abl and Aurora kinases
Brummendorf T J. Moll
Blood
(2008) 111(8), 4355-4364
abstract
First Cdc7 Kinase Inhibitors: Pyrrolopyridinones as Antitumor Agents. 1. Synthesis and Structure-Activity Relationships
Vanotti E, Amici R, Bargiotti A, Berthelsen J, Bosotti R, Ciavolella A, Cirla A, Cristiani C, D’Alessio R, Forte B, Martina K, Menichincheri M, Molinari A, Montagnoli A, Orsini P, Pillan A, Roletto F, Scolaro A, et al.
Journal of Medicinal Chemistry
(2008) 51, 487-501
abstract
NICOTINOYL AZIDE
Papeo GL, Posteri H, Vianello P, Varasi M
E.R.O.S. Encyclopedia of Reagents for Organic Synthesis
(2008), 1-6
The characterization of the first potent small molecule Cdc7 kinase inhibitor defines a novel class of anticancer agents
Montagnoli A, Valsasina B, Menichincheri M, Croci V, Tibolla M, Tenca PL, Rainoldi S, Brotherton D, Albanese C, Patton V, Alzani R, Ciavolella A, Sola F, Molinari A, Volpi D, Bensimon A, Vanotti E, Santocanale C
Nature Chemical Biology
(2008) 4 (6), 357-365
abstract
Aurora kinase inhibitors: identification and preclinical validation of their biomarkers
Carpinelli P, Moll J
Expert Opin Ther Targets
(2008), 12 (1), 69-80
abstract
Archivio 2007
Cdc7 is an active kinase in human cancer cells undergoing replication stress
Tenca P, Brotherton D, Montagnoli A, Rainoldi S, Albanese C, Santocanale C
Journal of Biological Chemistry
(2007) 282(1), 208-215
Abstract
Predicting the active doses in humans from animal studies: A novel approach in oncology
Rocchetti M, Simeoni M, Pesenti E, De Nicolao G, Poggesi I
Eur. J. Can.
(2007), 43(12):1862-1868
Abstract
Assessing and managing toxicities induced by kinase inhibitors
Castoldi RE, Pennella G, Saturno GS, Grossi P, Brughera M, Venturi M
Current Opinion in Drug Discovery & Development
(2007), 10(1):53-7
Abstract
Evaluation of a Physiological-Based Pharmacokinetic Modeling for Simulation of First Time in Animal Study
Germani M, Crivori P, Rocchetti M, Burton PS, Wilson AGE, Smith ME, Poggesi I
European J. of Pharmaceutical Sciences
(2007), 31:190-201
Abstract
Synthesis of PHA-690509 labelled with 14C
Fontana E, Giribone D, Feliciti C
J of Labelled Compounds and Radiopharm
(2007), 50:225-227
Abstract
Assessment of QT Liabilities in Drug Development: Regulatory Status and Current Practices
Arrigoni C, Crivori P
Cell Biology and Toxicology
(2007), 23(1):1-13
Abstract
De Novo Synthesis of thiophenes on a polymeric support
Traversone A, Brill W
Tetrahedron Letters
(2007) 48, 3535-3538
Abstract
Bortezomib inhibits nuclear factor-kB dependent survival and has potent in vivo activity in mesothelioma
Sartore-Bianchi A, Gasparri F, Galvani A, Nici L, Darnowski JW, Barbone D, Fennell DA, Gaudino G, Porta C, Mutti L
Clinical Cancer Research
(2007) 13, 19, 5942-5951
Abstract
Ongoing phase I and II studies of novel anthracyclines
Sessa C, Valota O, Geroni C
Cardiovascular Toxicology
(2007) 7, 75-79
Conclusion
Poly-Fluorinated Amino acids for Sensitive 19F NMR-Based Screening and Kinetic Measurements
Papeo GL, Giordano P, Brasca MG, Buzzo F, Caronni D, Ciprandi F, Mongelli N, Veronesi M, Vulpetti A, Dalvit C
J. Am. Chem. Soc.
(2007), 129
Abstract
Structures of the human eIF4E homologous protein, 4EHP, in its m(7)GTP-bound and Unliganded Forms
Rosettani P, Knapp S, Vismara S, Rusconi MG, Cameron A
Journal of Molecular Biology
(2007) 368, 3, 691-705
Summary
Antitumor Activity of Edotecarin in Breast Carcinoma Models
Ciomei M, Croci V, Stellari F, Amboldi N, Giavarini R, Pesenti E
Cancer Chemotherapy and Pharmacology
(2007) 60, 2, 229-235
Abstract
Magnetic Resonance Imaging and Histopathological Characterization of Prostate Tumors in TRAMP Mice as Model for Pre-Clinical Trials
De Grassi A, Russo M, Scanziani E, Giusti A, Ceruti R, Texido G, Pesenti E
The prostate
(2007) 67,396-404
Abstract
Cross platform microarray analysis for robust identification of differentially expressed genes
Bosotti R, Locatelli G, Healy S, Scacheri E, Sartori L, Mercurio C, Calogero R and Isacchi A
BMC Bioinformatics
(2007) 8, S5
Abstract
6-Substituted Pyrrolo[3,4-c]pyrazoles: An Improved Class of CDK2 Inhibitors
Brasca MG, Albanese C, Amici R, Ballinari D, Corti L, Croci V, Fancelli D, Fiorentini F, Nesi M, Orsini P, Orzi F, Pastori W, Perrone P, Pesenti E, Pevarello P, Riccardi-Sirtori F, Roletto F, Roussel P, Varasi M, Vulpetti A, Mercurio C
ChemMedChem
(2007), 2, 841-852
Abstract
Cell-cycle inhibitor profiling by high-content analysis
Gasparri F, Ciavolella A, Galvani A
Advances in Molecular Oncology (Book)
(2007) 604, 137-148
Abstract
Pyrazoles as efficient adenine-mimetic heterocucles for the discovery CDK inhibitors
Pevarello P, Vulpetti A
Inhibitors of cyclin-dependent kinases as anti-tumor agents (Book)
(2007) 15, 323-347
abstract
Development and Validation of In Silico Models for Estimating Drug Preformulation Risk in PEG400/Water and Tween80/Water Systems.
Crivori P, Morelli A, Pezzetta D, Poggesi I, Rocchetti M.
European J of Pharmaceutical Sciences
(2007), 32 (3):169-181
Abstract
PHA-739358, a potent inhibitor of Aurora kinases with a selective target inhibition profile relevant to cancer
Carpinelli P, Ceruti R, Giorgini ML, Cappella P, Gianellini L, Croci V, Degrassi A, Texido G, Rocchetti M, Vianello P, Rusconi L, Storici P, Zugnoni P, Arrigoni C, Soncini C, Alli C, Patton V, Marsiglio A, Ballinari D, Pesenti E, Fancelli D, Moll J.
Mol Cancer Ther.
2007 Dec;6(12 Pt 1):3158-68
Crystal structure of the T315I Abl mutant in complex with the aurora kinases inhibitor PHA-739358.
Modugno M, Casale E, Soncini C, Rosettani P, Colombo R, Lupi R, Rusconi L, Fancelli D, Carpinelli P, Cameron AD, Isacchi A, Moll J.
Cancer Research
Sep 1;67(17):7987-90.
Aurora kinase inhibitors: identification and preclinical validation of their biomarkers
Modugno M, Casale E, Soncini C, Rosettani P, Colombo R, Lupi R, Rusconi L, Fancelli D, Carpinelli P, Cameron AD, Isacchi A, Moll J.
Cancer Research
2007 Sep 1;67(17):7987-90
Identification of Mcm2 phosphorylation sites by S-phase regulating kinases
Montagnoli A, Valsasina B, Brotherton D, Troiani S, Rainoldi S, Tenca PL, Molinari A and Santocanale C
The Journal of Biological Chemistry
(2006) 281(5), 10281-10290
A practical synthesis of the major metabolite of a potent CDK2/cyclin A inhibitor
Nesi M, Borghi D, Brasca MG, Fiorentini F and Pevarello P
Bioorganic & Medicinal Chemistry Letters
(2006) 16, 3205-3208
Cyclin-Dependent Kinase 2 function in normal DNA repair and is a therapeutic target in BRCA1- deficient Cancers
Deans AJ, Khanna KK, McNees CJ, Mercurio C, Heierhorst J and McArthur GA
Cancer Research
(2006) 66(16), 8219-8226
PHA-680632, a novel Aurora kinases inhibitor with potent anti-tumoral activity
Soncini C, Carpinelli P, Gianellini L, Fancelli D, Vianello P, Rusconi L, Storici P, Zugnoni P, Pesenti E, Croci V, Ceruti R, Giorgini ML, Cappella P, Ballinari D, Sola F, Varasi M, Bravo R, Moll J
Clinical Cancer Research
(2006) 12(13), 4080-4089
NMR-Based Quality Control Approach for Identification of False Positives and False Negatives in High Throughput Screening
Dalvit C, Caronni D, Mongelli N, Veronesi M, Vulpetti A
Current Drug Discovery Technologies
(2006) 3, 115-124
Multiparametric cell-cycle analysis by automated microscopy
Gasparri F, Cappella P, Galvani A
J Biomol Screen
(2006) 6, 586-598
1,3,4-Oxadiazole formation as traceless release in solid phase organic synthesis
Cesarini S, Colombo N, Pulici M, Felder ER and Brill WK-D
Tetrahedon Letters
(2006) 62, 10223-10236
Inhibition of Protein-Protein Interactions: The Discovery of Druglike ?-Catenin Inhibitors by Combining Vvirtual and Biophysical Screening
Trosset J, Dalvit C, Knapp S, Fasolini M, Veronesi M, Mantegani S, Gianellini L, Catana C, Sundström M, Stouten P, Moll J
Proteins: Structure, Function and Bioinformatics
(2006) 64, 60-67
Structure-based Drug Design to the Discovery of New 2-aminothiazole CDK2 Inhibitors
Vulpetti A, Casale E, Roletto F, Amici R, Villa M, Pevarello P
Journal of Molecular Graphics and Modelling
(2006) 24, 341-348
Bicyclic Carbohydrate-Derived Scaffolds for Combinatorial Libraries
Cervi G, Peri F, Battistini C, Gennari C, Nicotra
Bioorganic & Medicinal Chemistry
(2006), 14, 3349-3367
1,4,5,6-Tetrahydropyrrolo [3,4-c]pyrazoles: Identification of a Potent Aurora Kinase Inhibitor with a Favorable Antitumor Kinase Inhibition Profile
Fancelli D, Moll J, Varasi M, Bravo R, Artico R, Berta D, Bindi S, Cameron A, Candiani I, Cappella P, Carpinelli P, Croci W, Forte B, Giorgini ML, Klapwijk J, Marsiglio A, Pesenti E, Rocchetti M, Roletto F, Severino D, Soncini C, Storici P, Tonani R,
J Med Chem
(2006) 49, 7247-7251
Multiparametric cell-cycle analysis by automated microscopy
Gasparri F, Cappella P, Galvani A
Journal of Biomolecular Screening
(2006) 11(6), 586-598
Compounds and methods for inhibiting mitotic progression
Fancelli D
Expert Opin Ther Patents
(2006) 16(8), 1179-1182
3-Amino-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: a new class of CDK2 inhibitors
Pevarello P, Fancelli D, Vulpetti A, Amici R, Villa M, Pittalà V, Vianello P, Cameron A, Ciomei M, Mercurio C, Bischoff JR, Roletto F, Varasi M and Brasca MG
Bioorganic and Medicinal Chemistry Letters
(2006) 16, 1084-1090
C-C- bond forming reactions
Brill WK.-D, Papeo G
Combinatorial Chemistry
(2006) 26,143-360
Cyclin-dependent kinase (CDK) inhibitors: a survey of the recent patent literature
Pevarello P, Villa M
Expert Opin Ther Patents
(2005) 15 (6), 675-703
PoInTree: a polar and interactive Phylogenetic tree
Carreras M, Gianti E, Sartori L, Plyte S, Isacchi A, Bosotti R
Gen Prot Bioinfo
(2005) 3(1), 58-61
Structure-based approaches to improve selectivity: CDK2 - GSK3b binding site analysis.
Vulpetti A, Crivori P, Cameron A, Bertrand J, Brasca G, D'Alessio R, Pevarello P
J Chem Inf Model
(2005), 45, 1282-1290
Trifluoroacetic Anhydride-Mediated Solid-Phase Version of the Robinson-Gabriel Synthesis of Oxazoles
Pulici M, Quartieri F, Felder ER
J Comb Chem
(2005) 7, 463-473
Potent and Selective Aurora-A Inhibitors Identified by the Expansion of a Novel Scaffold for Protein Kinase Inhibition
Fancelli D, Berta D, Bindi S, Cameron A, Cappella P, Carpinelli P, Catana C, Forte B, Giordano P, Giorgini ML, Mantegani S, Marsiglio A, Meroni M, Moll J, Pittalà V, Roletto F, Severino D, Soncini C, Storici P, Tonani R, Varasi M, Vulpetti A and Vian
J. Med. Chem.
(2005), 48, 3080-3084
3-Aminopyrazole inhibitors of CDK2/cyclin A as Antitumor agenys. 2. Lead Optimization
Pevarello P, Brasca MG, Orsini P, Traquandi G, Longo A, Nesi M, Orzi F, Piutti C, Sansonna P, Varasi M, Cameron A, Vulpetti A, Roletto F, Alzani R, Ciomei M, Albanese C, Pastori W, Marsiglio A, Pesenti E, Fiorentini F, Bischoff JR, Mercurio C
J Med Chem
(2005) 48, 2944-2956
Quantitative NMR in Synthetic and Combinatorial Chemistry
Rizzo V, Pinciroli V
Journal of Pharmaceutical & Biomedical Analysis
(2005) 8(5), 851-857
Searching for biomarkers of Aurora-A kinase activity: Identification of in vitro substrates through a modified KESTREL approach
Troiani S, Uggeri M, Moll J, Isacchi A, Kalisz HM, Rusconi L, Valsasina B
Journal of Proteome Research
(2005) 4, 1296-1303
Virtual screening to Enrich a Compound Collection with CDK2 inhibitors using Docking, Scoring and Consensus Scoring
Cotesta S, Giordanetto F, Trosset JY, Crivori P, Kroemer R, Stouten P, Vulpetti A
Proteins
(2005) 60, 629-643
Pyrazolyl-benzoxazole derivatives as protein kinase inhibitors. Design and validation of a combinatorial library
Berta D, Felder E, Villa M, Vulpetti A
Tetrahedron Letters
(2005) 61, 10801-10810
Regulation of the Wild-Type and Y1235D Mutant Met Kinase Activation
Cristiani C, Rusconi L, Perego R, Schiering N, Kalisz H, Knapp S, Isacchi A
Biochemistry
(2005) 44, 14110-14119
Benzodipyrazoles: a new class of potent CDK2 inhibitors
D'Alessio R, Bargiotti A, Betz S, Brasca G, Cameron A, Ermoli A, Marsiglio A, Polucci P, Roletto F, Tibolla M, Vazquez M, Vulpetti A, Pevarello P
Bioorganic and Medicinal Chemistry Letters
(2005) 15, 1315-1319
Traceless Solid-Phase Synthesis of 2-Amino-5-alkylidene-thiazol-4-ones
Pulici M, Quartieri F
Tetrahedron Letters
(2005) 46, 2387-2391
3-Acylaminopyrazole Derivatives via Regioselectively N-Protected 3-nitropyrazole
Orsini P, Traquandi G, Sansonna P, Pevarello P
Tetrahedron Letters
(2005) 46, 933-935
An Analysis of the Binding Modes of ATP-Competitive CDK2 Inhibitors as Revealed by X-Ray Structures of Protein-Inhibitor Complexes
Vulpetti A, Pevarello P
Current Medicinal Chemistry-Anti-Cancer Agents
(2005) 5, 561-573
4-demethoxy-3'-deamino-3'aziridinyl-4'methylsulphonyl-daunorubicin (PNU-159548): a new promising candidate for chemotherapeutic treatment of osteosarcoma patients
Pasello M, Hattinger CM, Stoico G, Manara MC, Benini S, Geroni C, Mercuri M, Scotlandi K, Picci P, Serra M
Eur J Cancer
(2005) 41, 2184-2195
Inhibitors of Aurora kinases for the treatment of cancer
Fancelli D, Moll J
Expert Opin Ther Patents
(2005), 15(9), 1169-1182
Sensitivity Improvement in the 19F NMR-based Screening Experiments: Theoretical Considerations and Experimental Applications
Dalvit C, Mongelli N, Papeo G, Giordano P, Veronesi M, Moskau D, Kümmerle R
Journal of the American Chemical Society
(2005) 127, 13380-13385
A New Glycociamidine Ring Precursor: Synthesis of (Z)-Hymenialdisine, (Z)-2-Debromohymenialdisine and (±)-endo-2-Debrormohyemialdisine
Papeo G, Posteri H, Borghi B, Varasi M
Organic Letters
(2005) 7(25), 5641-5644
Solid-phase synthesis of pyrido[2,3-d]pyrimidin-7-ones
Angiolini M, Fusar Bassini D, Gude M, Menichincheri M
Tetrahedron Letters
(2005) 46, 8749-8752
Total Synthesis of (±)-Cyclooroidin
Papeo G, Gomez-Zurita Frau MA, Borghi D, Varasi M
Tetrahedron Letters
(2005) 46, 8635-8638
Nicotinoyl Azide (NCA)-Mediated Mitsunoby Reaction: An Expedient One-Pot Transformation of Alcohols inot Azides
Papeo G, Posteri H, Vianello P, Varasi M
Synthesis
(2004) 17, 2886-2892
In vivo Assessment of Antiangiogenic Activity of SU6668 in an Experimental Colon Carcinoma Model
Marzola P, Degrassi A, Calderan L, Farace P, Crescimanno C, Nicolato E, Giusti A, Pesenti E, Terron A, Sbarbati A, Abrams T, Murray L, Osculati F
Clinical Cancer Research
(2004) 10, 739-750
Kinase selectivity profiling by inhibitor affinity chromatography
Valsasina B, Kalisz H, Isacchi A
Expert Review Proteomics
(2004) 1 (3), 89-101
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