Publications

2017

Amphoteric 2-(Sulfonylamino)Benzaldehydes, Secondary Amines and Isocyanides in the Multicomponent Synthesis of Elusive N-Alkyl-2,3-diaminoindoles
Giustiniano M., Pelliccia S., Sangaletti L., Meneghetti F., Amato J., Novellino E., Tron G.C.
Tetrahedron Lett., 2017, ASAP, -
An aryne-based three-component access to α-aroylamino amides
Serafini M., Griglio A., Viarengo S., Aprile S., Pirali T.
Org. Biom. Chem., 2017, 15, 6604-6612
Identification of a Potent Phosphoinositide 3-Kinase Pan Inhibitor Displaying a Strategic Carboxylic Acid Group and Development of Its Prodrugs
Pirali T., Ciraolo E., Aprile S., Massarotti A., Berndt A., Griglio A., Serafini M., Mercalli V., Landoni C., Cosimo Campa C., Margaria J.P., Silva R.L., Grosa G., Sorba G., Williams R., Hirsch E., Tron G.C.
ChemMedChem, 2017, 12, 1542-1554
TRPM8 receptor agonist compounds and uses thereof
Ferrer Montiel A., Fernandez Carvajal A., Belmonte M.C., Gallar M.J., De La Torre R., Genazzani R., Tron G.C., Mercalli V.
PCT Int. Appl., 2017, WO20171256, -
A Fast Route for the Synthesis of Tetrazolyl Oximes by a Novel Multicomponent Reaction between Z-Chlorooximes, Isocyanides and Trimethylsilyl Azide
Giustiniano M., Pelliccia S., Muñoz-Garcia A.B., Pavone M., Pagano B., Galli U., Novellino E., Tron G.C.
Tetrahedron Lett., 2017, 58, 3549-3553
Identification of Novel Triazole-Based Nicotinamide Phosphoribosyltransferase (NAMPT) Inhibitors Endowed with Anti-Proliferative and Anti-Inflammatory Activity
Travelli C., Aprile S., Rahimian R., Grolla A.A., Rogati F., Bertolotti M., Malagnino F., Di Paola R., Impellizzeri D., Fusco R., Mercalli V., Massarotti A., Stortini G., Terrazzino S., Del Grosso E., Fakhfouri G., Pia Troiani M., Alisi M.A., Grosa G., Sorba G., Canonico P.L., Orsomando G., Cuzzocrea S., Genazzani A.A., Galli U., Tron G.C.
J. Med. Chem., 2017, 60, 1768-1792
N–N bond formation in Ugi processes: from nitric acid to libraries of nitramines
Mercalli V., Nyadanu A., Cordier M., Tron G.C., Grimaud L.,El Kaim L.
Chem. Commun., 2017, 53, 2118-2121
To each his own: isonitriles for all flavors. Functionalized isocyaides as valuable tools in organic synthesis
Giustiniano M., Basso A., Mercalli V., Massarotti A., Novellino E., Tron G.C., Zhu J.
Chem. Soc. Rev., 2017, 46, 1295-1357

2016

A Successful Replacement of Phenols with Isocyanides in the Bargellini Reaction: Synthesis of 3-Carboxamido-Isobutyric acids
Giustiniano M., Pelliccia S., Galli U., Amato J., Travagin F., Novellino E., Tron G.C.
J. Org. Chem., 2016, 81, 11467-11471
BDNF Val66Met and clinical response to antipsychotic drugs: a systematic review and meta-analysis
Cargnin S., Massarotti A., Terrazzino S.
Eu. Psychiatry, 2016, 33, 45-53
The Adverse Outcome Pathway (AOP) for chemical binding to tubulin in oocytes leading to aneuploid offspring
Marchetti F., Massarotti A., Yauk C.L., Pacchierotti F., Russo A.
Environ. Mol. Mutagen., 2016, 57, 87-113
In silico-driven multicomponent synthesis of 4,5- and 1,5-disustituted imidazoles as indoleamine 2,3-dioxygenase inhibitors
Fallarini S., Massarotti A., Gesù A., Giovarruscio S., Coda Zabetta G., Bergo R., Giannelli B., Brunco A., Lombardi G., Sorba G., Pirali T.
Med. Chem. Commun., 2016, 7, 409-419

2015

The Guareschi Pyridine Scaffold as a Valuable Platform for the Identification of Selective PI3K Inhibitors
Galli U., Ciraolo E., Massarotti A., Margaria J.P., Sorba G., Hirsch E., Tron G.C.
Molecules, 2015, 20, 17275-17287
Identification of a novel NAMPT inhibitor by combinatorial click chemistry and chemical refinement
Theeramunkong S., Galli U., Grolla A.A., Caldarelli A., Travelli C., Massarotti A., Troiani M.P., Alisi M.A., Orsomando G., Genazzani A.A., Tron G.C
Med. Chem. Commun., 2015, 6, 1891-1897
Design, Synthesis and Biological Evaluation of Combretabenzodiazepines: a Novel Class of Antitubulin Agents
Galli U., Travelli C., Aprile S., Arrigoni E., Torretta S., Grosa G., Massarotti A., Sorba G., Canonico P.L., Genazzani A.A., Tron G.C.
J. Med. Chem., 2015, 58, 1345-1357
Synthesis of Heteroarylogous 1H-Indole-3-Carboxamidines Through a Three-Component Interrupted Ugi Reaction
La Spisa F., Meneghetti F., Pozzi B., Tron G.C.
SYNTHESIS, 2015, 47, 489-496

2014

Inhibitors of nicotinamide phosphoribosyltransferase, compositions, products and uses thereof
Genazzani A.A., Tron G.C., Galli U., Travelli C., Cuzzocrea S., Grosa G., Sorba G., Canonico P.L.
PCT Int. Appl., 2014, WO2014178001 (A1), -
Solution phase parallel synthesis of aryloxyimino amides via a novel multicomponent reaction among aromatic (Z)-chlorooximes, isocyanides and electron deficient phenols
Mercalli V., Giustiniano M., Del Grosso E., Varese M., Cassese H., Massarotti A., Novellino E., Tron G.C.
ACS Comb. Sci., 2014, 16, 602-605
Synthesis of Aminocarbonyl N-Acylhydrazones by a Three-Component Reaction of Isocyanides, Hydrazonoyl Chlorides, and Carboxylic Acids
Giustiniano M., Meneghetti F., Mercalli V., Varese M., Giustiniano F., Novellino E., Tron G.C.
Org. Lett., 2014, 16, 5332-5335
Are 1,4- and 1,5-disubstituted-1,2,3-triazoles good pharmacophoric groups?
Massarotti A., Aprile S., Mercalli V., Del Grosso E., Grosa G., Sorba G., Tron G.C.
ChemMedChem, 2014, 9, 2497-2508
Reaction Between (Z)-Arylchlorooximes and alpha-Isocyanoacetamides: a Procedure For The Synthesis of Aryl-alpha-Ketoamide amides
Giustiniano M., Mercalli V., Cassese H., Di Maro S., Galli U., Novellino E., Tron G.C.
J. Org. Chem., 2014, 79, 6006-6014
The Nef Reaction of Isocyanides
La Spisa F., Tron G.C., El Kaïm L.
SYNTHESIS, 2014, 46, 829-841
ZINClick: a database of 16 million novel, patentable and readily synthesizable 1,4-disubstituted triazoles
Massarotti A., Brunco A., Sorba G., Tron G.C.
J. Chem. Inf. Model, 2014, 54, 396-406
Small molecule inhibitors of West Nile virus
Elseginy S.A., Massarotti A., Nawwar G.A., Amin K.M., Brancale A.
Antivir. Chem. Chemother., 2014, 23, 179-187

2013

Isocyanide-Mediated Multicomponent Synthesis of C-Oximinoamidines
Mercalli V., Meneghetti F., Tron G.C.
Org. Lett., 2013, 15, 5902-5905
Medicinal Chemistry of Nicotinamide Phosphoribosyltransferase (NAMPT) inhibitors
Galli U., Travelli C., Massarotti A., Fakhfouri G., Rahimian R., Tron G.C., Genazzani A.A.
J. Med. Chem., 2013, 56, 6279-6296
Off the beaten track: the use of secondary amines in the Ugi reaction
Tron G.C.
Eur. J. Org. Chem., 2013, 2013, 1849-1859
Computer-aided identification, design and synthesis of a novel series of compounds with selective antiviral activity against chikungunya virus
Bassetto M., De Burghgraeve T., Delang L., Massarotti A., Coluccia A., Gatti V., Colombano G., Sorba G., Silvestri R., Tron G.C., Neyts J., Leyssen P., Brancale A.
Antvir. Res., 2013, 98, 12-18
A Concise Synthesis of Pyrazole Analogues of Combretastatin A1 as Potent Antitubulin Agents
Zaninetti R., Cortese S.V., Aprile S., Massarotti A., Canonico P.L., Sorba G., Grosa G., Genazzani A.A., Pirali T.
ChemMedChem, 2013, 8, 633-643
Parallel synthesis of “click” chalcones as antitubulin agents
Utsintong M., Massarotti A., Caldarelli A., Theeramunkong S.
Med. Chem., 2013, 9, 510-516
Nicotinamide phosphoribosyltransferase (NAMPT) is over-expressed in melanoma lesions
Maldi E., Travelli C., Caldarelli1 A., Agazzone N., Cintura S., Galli U., Scatolini M., Ostano P., Miglino B., Chiorino G., Boldorini R., Genazzani A.A.
Pigment Cell Melanoma Res, 2013, 26, 144-146

2012

An efficient synthesis of symmetric and unsymmetric bis-(β-aminoamides) via Ugi multicomponent reaction
La Spisa F., Feo A., Mossetti R., Tron G.C.
Org. Lett., 2012, 14, 6044-6047
Identification of a sirtuin 3 inhibitor that displays selectivity over sirtuin 1 and 2
Galli U., Mesenzani O., Coppo C., Sorba G., Canonico P.L., Tron G.C., Genazzani A.A.
Eu. J. Med. Chem., 2012, 55, 58-66
Quinolin-4 (1h)-one derivatives as inhibitors of phosphatidylinositol 3-kinases
Sorba G.,Tron G.C., Galli U., Massarotti A., Hirsch E., Ciraolo E., Pirali T.
PCT Int. Appl., 2012, WO 2012073, -
PI3K keeps the balance between metabolism and cancer
Braccini L., Ciraolo E., Martini M., Pirali T., Germena G., Rolfo K., Hirsch E.
Adv. Biol. Reg., 2012, 52, 389-405
Haptic-Driven applications to Molecular Modelling: State of the Art and Perspectives
Ricci A., Anthopoulos A., Massarotti A., Grimstead I., Brancale A.
Future Med. Chem., 2012, 4, 1219-1228
The NAMPT inhibitor FK866 reverts the damage in spinal cord injury
Esposito E., Impellizzeri D., Mazzon E., Fakhfouri G., Rahimian R., Travelli C., Tron G.C., Genazzani A.A., Cuzzocrea S.
J. Neuroinflammation, 2012, 9, 66-77
De novo computer-aided design of novel antiviral agents
Massarotti A., Coluccia A., Sorba G., Silvestri R., Brancale A.
Drug Discovery Today: Technologies, 2012, 9, e213-e218
Transition metal-free direct arylation of anilines
Pirali T., Zhang F., Miller A.H., Head J.L., McAusland D., Greaney M.F.
Angew. Chem. Int. Ed., 2012, 51, 1006-1009
The tubulin colchicine domain: a molecular modelling perspective
Massarotti A., Coluccia A., Silvestri R., Sorba G., Brancale A.
ChemMedChem, 2012, 7, 33-42

2011

Identification of novel antitubulin agents by using a virtual screening approach based on a 7-point pharmacophore model of the tubulin Colchi-site
Massarotti A., Theeramunkong S., Mesenzani O., Caldarelli A., Genazzani A.A., Tron G.C.
Chem. Biol. Drug Des., 2011, 78, 913-922
Pietro Biginelli: The Man Behind the Reaction
Tron G.C., Minassi A., Appendino G.
Eur. J. Org. Chem., 2011, 2011, 5541-5550
Regioselective Suzuki coupling of dihaloheteroaromatic compounds as a rapid strategy to synthesize potent rigid combretastatin analogues
Theeramunkong S., Caldarelli A., Massarotti A., Aprile S., Caprioglio D., Zaninetti R., Teruggi A., Pirali T., Grosa G., Tron G.C., Genazzani A.A.
J. Med. Chem., 2011, 54, 4977-4986
Reciprocal potentiation of the antitumoral activities of FK866, an inhibitor of nicotinamide phosphoribosyltransferase, and etoposide or cisplatin in neuroblastoma cells
Travelli C., Drago V., Maldi E., Kaludercic N., Galli U., Boldorini R., Di Lisa F., Tron G.C., Canonico P.L., Genazzani A.A.
J. Pharm. Exp. Therap., 2011, 338, 829-840
Imides: Forgotten Players in the Ugi reaction. One pot multicomponent synthesis of quinazolinones
Mossetti R., Pirali T., Saggiorato D., Tron G.C.
Chem. Comm., 2011, 47, 6966-6968
Groebke multicomponent reaction and subsequent nucleophilic aromatic substitution for a convenient synthesis of 3,8-diaminoimidazo[1,2-a]pyrazines as potential kinase inhibitors
Guasconi M., Lu X., Massarotti A., Caldarelli A., Ciraolo E., Tron G.C., Hirsch E., Sorba G., Pirali T.
Org. Biomol. Chem., 2011, 9, 4144-4149
A novel a-isocyanoacetamide-based three-component reaction for the synthesis of dialkyl 2-acyl-5-aminofuran-3,4-dicarboxylates
Mossetti R., Caprioglio D., Colombano G., Tron G.C., Pirali T.
Org. Biomol. Chem., 2011, 9, 1627-1631
Replacement of the double bond of antitubulin chalcones with triazoles and tetrazoles: synthesis and biological evaluation
Mesenzani O., Massarotti A., Giustiniano M., Pirali T., Bevilacqua V., Caldarelli A., Canonico P.L., Sorba G., Novellino E., Genazzani A.A., Tron G.C.
Bioorg. Med. Chem. Lett., 2011, 21, 764-768

2010

A Practical Synthesis of 5-Aroyl-1-aryltetrazoles Using an Ugi-Like 4-Component Reaction Followed by a Biomimetic Transamination
Giustiniano M., Pirali T., Massarotti A., Biletta B., Novellino E., Campiglia P., Sorba G., Tron G.C.
Synthesis, 2010, 23, 4107-4118
Essential role of the p110beta subunit of phosphoinositide 3-OH kinase in male fertility
Ciraolo E., Morello F., Hobbs R.M., Wolf F., Marone R., Iezzi M., Lu X., Mengozzi G., Altruda F., Sorba G., Guan K., Pandolfi P.P., Wymann M.P., Hirsch E.
Mol. Biol. Cell., 2010, 21, 704-711
Stereoselective synthesis of trans-beta-lactams by palladium-catalysed carbonylation of vinyl aziridines
Fontana F., Tron G.C., Barbero N., Ferrini S., Thomas S.P., Aggarwal V.K.
Chem. Commun., 2010, 46, 267-269
A novel potent nicotinamide phosphoribosyltransferase inhibitor synthesized via click chemistry
Colombano G., Travelli T., Galli U., Caldarelli A., Chini M.G., Canonico P.L., Sorba G., Bifulco G., Tron G.C., Genazzani A.A.
J. Med. Chem., 2010, 53, 616-623
Synthesis, molecular docking and biological evaluation as HDAC inhibitors of cyclopeptide mimetics by a tandem three-component reaction and intramolecular [3+2] cycloaddition
Pirali T., Faccio V., Mossetti R., Grolla A.A., Di Micco S., Bifulco G., Genazzani A.A., Tron G.C.
Mol. Divers., 2010, 14, 109-121

2009

Synthesis of Passerini-Ugi Hybrids by a Four-Component Reaction Using the Glycolaldehyde Dimer
Mossetti R., Pirali T., Tron G.C.
J. Org. Chem., 2009, 74, 4890-4892
Synthesis, biological evaluation, and molecular docking of Ugi products containing a zinc-chelating moiety as novel inhibitors of histone deacetylases
Grolla A.A., Podestà V., Chini M.G., Di Micco S., Vallario A., Genazzani A.A., Canonico P.L., Bifulco G., Tron G.C., Sorba G., Pirali T.
J. Med. Chem., 2009, 52, 2776-2785

2008

A coincise entry into non-symmetrical alkyl polyamines
Pirali T., Callipari G., Ercolano E., Genazzani A.A., Giovenzana G.B., Tron G.C.
Org. Lett., 2008, 10, 4199-4202
Characterization of NAD uptake in mammalian cells
Billington R.A., Travelli C., Ercolano E., Galli U., Roman C., Grolla A.A., Canonico P.L., Condorelli F., Genazzani A.A.
J. Biol. Chem., 2008, 283, 6367-6374
Solution-phase parallel synthesis and biological evaluation of combretatriazoles
Cafici L., Pirali T., Condorelli F., Del Grosso E., Massarotti A., Sorba G., Canonico P.L., Tron G.C., Genazzani A.A.
J. Comb. Chem., 2008, 10, 732-740
Triazole-modified histone deacetylase inhibitors as a rapid route to drug discovery
Pirali T., Pagliai F., Mercurio C., Boggio R., Canonico P.L., Sorba G., Tron G.C., Genazzani A.A.
J. Comb. Chem., 2008, 10, 624-627
Synthesis and biological evaluation of isosteric analogues of FK866, an inhibitor of NAD salvage
Galli U., Ercolano E., Carraro L., Blasi Roman C.R., Sorba G., Canonico P.L., Genazzani A.A., Tron G.C., Billington R.A.
ChemMedChem, 2008, 3, 771-779
Click chemistry reactions in medicinal chemistry: applications of the 1,3-dipolar cycloaddition between azides and alkynes
Tron G.C., Pirali T., Billington R., Canonico P.L., Sorba G., Genazzani A.
Med. Res. Rev., 2008, 28, 278-308

2007

In vitro metabolism study of combretastatin A-4 in rat and human liver microsome
Aprile S., Del Grosso E., Tron G.C., Grosa G.
Drug Metab. Dispo., 2007, 35, 2252-2261
Replacement of the lactone moiety on podophyllotoxin and steganacin analogues with a 1,5-disubstituted 1,2,3-triazole via ruthenium-catalyzed click chemistry
Imperio D., Pirali T., Galli U., Pagliai F., Cafici L., Canonico P.L., Sorba G., Genazzani A.A., Tron G.C.
Bioorg. Med. Chem., 2007, 15, 6748-6757
Estrogenic analogues synthesized via click chemistry
Pirali T., Gatti S., Di Brisco R., Tacchi S., Zaninetti R., Brunelli E:, Massarotti A., Sorba G., Canonico P.L., Moro L., Genazzani A.A., Tron G.C., Billington R.A.
ChemMedChem, 2007, 2, 437-440
Design, synthesis, and biological evaluation of new (2E,6E)-10-(dimethylamino)-3,7-dimethyl-2,6-decadien-1-ol ethers as inhibitors of human and Trypanosoma cruzi oxidosqualene cyclase
Galli U., Oliaro-Bosso S., Taramino S., Venegoni S., Pastore E., Tron G.C., Balliano G., Viola F., Sorba G.
Bioorg. Med. Chem. Lett., 2007, 17, 220-224

2006

Synthesis and cytotoxic evaluation of combretafurans, potential scaffolds for dual-action antitumoral agents
Pirali T., Busacca S., Beltrami L., Imovilli D., Pagliai F., Miglio G., Massarotti A., Verotta L., Tron G.C., Sorba G., Genazzani A.A.
J. Med. Chem., 2006, 49, 5372-5376
Medicinal chemistry of combretastatin A-4: present and future directions
Tron G.C., Pirali T., Sorba G., Pagliai F., Busacca S., Genazzani A.A.
J. Med. Chem., 2006, 49, 3033-3044
Split the primary amine in two: secondary diamines may play the role of the primary amine in the Ugi 4CR
Giovenzana G.B., Tron G.C., Di Paola S., Menegotto I.G., Pirali T.
Angew. Chem. Int. Ed., 2006, 45, 1099-1102
Rapid synthesis of triazole-modified resveratrol analogues via click chemistry
Pagliai F., Pirali T., Del Grosso E., Di Brisco R., Tron G.C., Sorba G., Genazzani A.A.
J. Med. Chem., 2006, 49, 467-470

2005

Synthesis and biological activity of mustard derivatives of combretastatins
Coggiola B., Pagliai F., Allegrone G., Genazzani A.A., Tron G.C.
Bioorg. Med. Chem. Lett., 2005, 15, 3551-3554
Synthesis and cytotoxic evaluation of combretafurazans
Tron G.C., Pagliai F., Del Grosso E., Genazzani A.A., Sorba G.
J. Med. Chem., 2005, 48, 3260-3268
Role of the nicotinic acid group in NAADP receptor selectivity
Billington R.A., Tron G.C., Reichenbach S., Sorba G., Genazzani A.A.
Cell Calcium, 2005, 37, 81-86
Synthetic Medicinal Chemistry group - Dipartimento di Scienze del Farmaco - Università degli Studi del Piemonte Orientale "A. Avogadro"
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