Biochemical and structural analysis of a cytosolic sulfotransferase of the malaria vector Anopheles gambiae overexpressed in the reproductive tissues

Curr Res Struct Biol 2022, 4, 246-255

Verza A., Miggiano R., ..., Del Grosso E., Galli U., Rizzi M., Rossi F.

Synthesis of Novel Lipophilic Polyamines via Ugi Reaction and Evaluation of Their Anticancer Activity

Molecules 2022, 27, 6218-

Nichugovskiy A., ..., Tron G.C., Maslov M.

In-water synthesis of isocyanides under micellar conditions

Green Chemistry 2022, 24, 7022-7028

Brunelli F., Aprile S., Russo C., Giustiniano M., Tron G.C.

Visible-light photocatalytic metal-free multicomponent Ugi-like chemistry

Green Chem. 2022, 24, 3993-4003

Russo C., Graziani G., Cannalire R., Tron G.C., Giustiniano M.

Photomicellar Catalyzed Synthesis of Amides from Isocyanides: Optimization, Scope, and NMR Studies of Photocatalyst/Surfactant Interactions

ACS Org. Inorg. Au 2022, 2, 66-74

Cannalire R., Santoro F., Russo C., Graziani G., Tron G.C., Carotenuto A., Brancaccio D., Giustiniano M.

Visible-Light Photoredox Catalysis in Water

J. Org. Chem. 2022, ASAP, -

Russo C., Brunelli F., Tron G.C., Giustiniano M.

Domino synthesis of 5-aminoimidazoles from Strecker multicomponent adducts via ytterbium-promoted isocyanide insertion/5-exo-dig cyclization

Mol. Div. 2022, , -

Cannalire R., Russo C., Paolo Luciano, Bruno Cerra, Antimo Gioiello, Francesca Brunelli, Gian Cesare Tron & Mariateresa Giustiniano

The Dark Side of Isocyanides: Visible-Light Photocatalytic Activity in the Oxidative Functionalization of C(sp3)–H Bonds

J. Org. Chem. 2021, 86, 18117-18127

Russo C., Amato J., Tron G.C., Giustiniano M.

PI(3,4)P2-mediated cytokinetic abscission prevents early senescence and cataract formation

Science 2021, 374, 1339-

Gulluni F., Prever L., Li H., ..., Massarotti A., ..., Hirsch E.

Visible-Light Photocatalytic Ugi/Aza-Wittig Cascade towards 2-Aminomethyl-1,3,4-oxadiazole Derivatives

Synthesis 2021, 53, 4419-4427

Russo C, Cannalire R., Luciano P., Brunelli F., Tron G.C., Giustiniano M.

Recent Advances in the Synthesis of Polyamine Derivatives and Their Applications

Molecules 2021, 26, 6579-

Nichugovskiy A., Tron G.C., Maslov M

Synthesis and Characterization of Bis-Triazolyl-Pyridine Derivatives as Noncanonical DNA-Interacting Compounds

Int. J. Mol. Sci. 2021, 22, 11959-

Di Porzio A., Galli U., Amato J., ..., Tron G.C., Randazzo A.

Multicomponent reaction between (Z)-chloroximes, isocyanides and NH-heterocyclic rings

Tetrahedron Letters 2021, 86, -

Brunelli F., Russo C., Giustiniano M, Tron G.C.

The [1,2,4]Triazolo[4,3-a]pyridine as a New Player in the Field of IDO1 Catalytic Holo-Inhibitors

ChemMedChem 2021, 16, 3439-3450

Fallarini S., Bhela I.P., Aprile S., Torre E., Ranza A., Orecchini E., Panfili E., Pallotta M.T., Massarotti A., Serafini M., Pirali T.

Medicinal Chemistry of Isocyanides

Chem Rev. 2021, 121, 10742-10788

Massarotti A., Brunelli F., Aprile S., Giustiniano M., Tron G.C.

Icilio Guareschi and his amazing "1897 reaction"

Beilstein J Org Chem 2021, 17, 1335-1351

Tron G.C., Minassi A., Sorba G., Fausone M., Appendino G.

Tritylamine as an Ammonia Surrogate in the Ugi Reaction Provides Access to Unprecedented 5-Sulfamido Oxazoles Using Burgess-type Reagents

Org Lett. 2021, 23, 3610-3614

Bhela I.P., Serafini M., Del Grosso E., Tron G.C., Pirali T.

1,2,4-Oxadiazole-Bearing Pyrazoles as Metabolically Stable Modulators of Store-Operated Calcium Entry

ACS Med Chem Lett 2021, 12, 640-646

Aprile S., Riva B., Bhela I.P., Cordero-Sanchez C., Avino G., Genazzani A.A., Serafini M., Pirali T.

What's in a Name? Drug Nomenclature and Medicinal Chemistry Trends using INN Publications

J. Med. Chem. 2021, 64, 4410-4429

Serafini M., Cargnin S., Massarotti A., Tron G.C., Pirali T., Genazzani A.A.

Moonlighting Proteins Are Important Players in Cancer Immunology

Front. Immunol. 2021, 11, 613069-

Adamo A., Frusteri C., Pallotta M.T., Pirali T., Sartoris S., .Ugel S

The 115 Year Old Multicomponent Bargellini Reaction: Perspectives and New Applications

Molecules 2021, 26, 558-

Serafini M., Murgia I., Giustiniano M., Pirali T., Tron G.C.

Therapeutic Peptides for the Treatment of Cystic Fibrosis: Challenges and Perspectives

Eu. J. Med. Chem. 2021, 213, 113191-

Sala V., Cnudde S., Murabito A., Massarotti A., Hirsch E., Ghigo A.

Visible light photocatalysis in the late-stage functionalization of pharmaceutically relevant compounds

Chem. Soc. Rev. 2021, ASAP, -

Cannalire R., Pelliccia S., Sancineto L., Novellino E., Tron G.C., Giustiniano M

Click 1,2,3-triazoles in drug discovery and development: from the flask to the clinic?

Advances in Heterocyclic Chemistry 2021, ASAP, -

Serafini M., Pirali T., Tron G.C.

The SNAP-tag technology revised: an effective chemo-enzymatic approach by using a universal azide-based substrate

J Enzyme Inhib Med Chem 2021, 36, 85-97

Merlo R., Caprioglio D., Cillo M., Valenti A., Mattossovich R., Morrone C., Massarotti A., Rossi F., Miggiano R., Leonardi A., Minassi A., Perugino G.

Visible-Light Photocatalytic Functionalization of Isocyanides for the Synthesis of Secondary Amides and Ketene Aminals

J. Org. Chem. 2020, 85, 14077-14086

Cannalire R., Amato J., Summa V., Novellino E., Tron G.C., Giustiniano M.

Psychotropic drugs show anticancer activity by distrupting mitochondrial and lysosomal function

Front. Oncol. 2020, , -

Varalda M., Antona A., Bettio V., Roy K., Vachanaram A.R., Yellenki V., Massarotti A., Baldanzi G., Capello D.

Recent Advances in NAMPT Inhibitors: A Novel Immunotherapic Strategy

Front. Pharmacol. 2020, , -

Galli U., Colombo G., Travelli C., Tron G.C., Genazzani A.A., Grolla A.A.

The Essential Medicinal Chemistry of Essential Medicines

J. Med. Chem. 2020, 63, 10170-10187

Serafini M., Cargnin S., Massarotti A., Pirali T., Genazzani A.A.

Discovery of Highly Potent Benzimidazole Derivatives as Indoleamine 2,3-Dioxygenase-1 (IDO1) Inhibitors: From Structure-Based Virtual Screening to in Vivo Pharmacodynamic Activity

J. Med. Chem. 2020, 63, 3047-3065

Serafini M., Torre E., Aprile S., Del Grosso E., Gesù A., Griglio A., Colombo G., Travelli C., ..., Massarotti A., Pirali T., Fallarini S.

The metabolic fate of the isocyanide moiety. Are isocyanides pharmacophore groups neglected by medicinal chemists?

Chem. Res. Toxicol. 2020, 33, 955-966

Galli U., Tron G.C., Purghè B., Grosa G., Aprile S.

A nicotinamide phosphoribosyltransferase–GAPDH interaction sustains the stress-induced NMN/NAD+ salvage pathway in the nucleus

J. Biol. Chem 2020, 295, 3635-3651

Grolla A., Miggiano R., ..., Galli U., Del Grosso E., ..., Genazzani A.A., Garavaglia S.

Data on metabolic stability, aqueous solubility and CYP inhibition of novel triazole-based nicotinamide phosphoribosyltransferase (NAMPT) inhibitors

Data in brief 2020, 28, 105034-

Aprile S., Galli U., Tron G.C., Del Grosso E., Travelli C., Grosa G.

Photocatalytic Isocyanide-based Multicomponent Domino Cascade Towards the Stereoselective Formation of Iminofurans

J. Org. Chem. 2020, 85, 1981-1990

Pelliccia S., Alfano A.I., Luciano P., Novellino E., Massarotti A., Tron G.C., Ravelli D., Giustiniano M.

Bio-Inspired Dual-Selective BCL-2/c-MYC G-Quadruplex Binders: Design, Synthesis, and Anticancer Activity of Drug-like Imidazo[2,1-i]purine Derivatives

J. Med. Chem. 2020, 63, 2035-2050

Pelliccia S., Amato J., Capasso D., Di Gaetano S., Massarotti A., Piccolo M., Irace C., Tron G.C., Pagano B., Randazzo A., Novellino E., Giustiniano M.

Structure activity relationship studies on Amb639752: toward the identification of a common pharmacophoric structure for DGKα inhibitors

J Enzyme Inhib Med Chem 2020, 35, 96-108

Velnati S., Massarotti A., Antona A., Talmon M., Fresu L.G., Galetto A.S., Capello D., Bertoni A., Mercalli V., Graziani A., Tron G.C., Baldanzi G.

A luminal EF-hand mutation in STIM1 in mice causes the clinical hallmarks of tubular aggregate myopathy

Dis Model Mech 2020, 13, -

Cordero-Sanchez C., Riva B., Reano S., Clemente N., Zaggia I., Ruffinatti F.A., Potenzieri A., Pirali T., Raffa S., Sangaletti S., Colombo M.P., Bertoni A., Garibaldi M., Filigheddu N., Genazzani A.A.

Aryl azides as forgotten electrophiles in the Van Leusen reaction: a multicomponent transformation affording 4-tosyl-1-arylimidazoles

J. Org. Chem. 2019, 84, 16299-16307

Necardo C., Alfano A.I., Del Grosso E., Pelliccia S., Galli U., Novellino E., Meneghetti F., Giustiniano M., Tron G.C.

A primer of deuterium in drug design

Future Med Chem. 2019, 11, 2039-2042

Cargnin S., Serafini M., Pirali T.

Soft drugs for dermatological applications: recent trends

Drug Discovery Today 2019, 24, 2234-2246

Aprile S., Serafini M., Pirali T.

Identification of potent triazolylpyridine nicotinamide phosphoribosyltransferase (NAMPT) inhibitors bearing a 1,2,3-triazole tail group

Eur. J. Med. Chem. 2019, 181, 111576-

Travelli C., Aprile S., ..., Grosa G., Genazzani A., Tron G.C., Galli U.

α-Amino Acids as Synthons in the Ugi-5-Centers-4-Components Reaction: Chemistry and Applications

Symmetry 2019, 11, 798-

Pelliccia S., Alfano I.A., Galli U., Novellino E., Giustiniano M., Tron G.C.

Study of Anopheles gambiae 3-hydroxykynurenine transaminase activity and inhibition by LC-MS/MS method

JPBA 2019, 173, 154-161

Canavesi R., Miggiano R., Stella M., Galli U., Rossi F., Rizzi M., Del Grosso E.

Exploiting the Nucleophilicity of the Nitrogen Atom of Imidazoles: One-Pot Three-Component Synthesis of Imidazo-Pyrazines

Molecules 2019, 24, 1959-

Galli U., Hysenlika R., Meneghetti F., Del Grosso E., Pelliccia S., Novellino E., Giustiniano M., Tron G.C.

Synthesis, Docking and Biological Evaluation of a Novel Class of Imidazothiazoles as IDO1 Inhibitors

Molecules 2019, 24, 1874-

Serafini M., Torre E., Aprile S., Massarotti A., Fallarini S., Pirali T.

Drug Discovery for Soft Drugs on TRPV1 and TRPM8 Channels Using the Passerini Reaction

Methods Mol Biol. 2019, 1987, 207-221

Pirali T., Galli U., Serafini M., Griglio A., Genazzani A.A., Tron G.C.

Nicotinamide Phosphoribosyltransferase (NAMPT) acts as a metabolic gate for mobilization of myeloid-derived suppressor cells

Cancer Res. 2019, 79, -

Travelli C., Consonni F.M., Sangaletti S., Storto M., Morlacchi S., Grolla A.A., Galli U., Tron G.C., Portararo P., Rimassa L., Pressiani T., Mazzone M., Trovato R., Ugel S., Bronte V., Tripodo C., Colombo M.P., Genazzani A.A., Sica A.

Applications of deuterium in medicinal chemistry

J. Med. Chem. 2019, 62, 5276-5297

Pirali T., Serafini M., Cargnin S., Genazzani A.A.

Identification of a novel DGKα Inhibitor for XLP-1 Therapy by Virtual Screening

Eu. J. Med. Chem. 2019, 164, 378-390

Velnati S., Ruffo E., Massarotti A., Talmon M., Sandeep Varma K.S., Gesù A., Fresu L.G., Snow A.L., Bertoni A., Capello D., Tron G.C., Graziani A., Baldanzi G.

ZINClick v.18: Expanding Chemical Space of 1,2,3-Triazoles

J. Chem. Inf. Model 2019, 59, 1697-1702

Levré D., Arcisto C., Mercalli V., Massarotti A.

Inhalation of the prodrug PI3K inhibitor CL27c improves lung function in asthma and fibrosis

Nat. Commun. 2018, 9, 5232-

Campa C.C., Silva R.L., Margaria J.P., Pirali T., Mattos M.S., Kraemer L.R., Reis D.C., Grosa G., Copperi F., Dalmarco E.M., Lima-Júnior R.C.P., Aprile S., Sala V., Dal Bello F., Prado D.S., Alves-Filho J.C., Medana C., Cassali G.D., Tron G.C., Teixeira M.M., Ciraolo E., Russo R.C., Hirsch E.

Pyrtriazoles, a Novel Class of Store-Operated Calcium Entry Modulators: Discovery, Biological Profiling and In Vivo Proof-of-Concept Efficacy in Acute Pancreatitis

J. Med. Chem. 2018, 61, 9756-9783

Riva B., Griglio A., Serafini M., Cordero Sanchez C., Aprile S., Di Paola R., Gugliandolo E., Alansary D., Biocotino I., Lim D., Grosa G., Galli U., Niemeyer B., Sorba G., Canonico P.L., Cuzzocrea S., Genazzani A.A., Pirali T.

On-water pyrrolidine-mediated domino synthesis of 2-iminoisatins

Green Chem. 2018, 20, 3912-3915

Pelliccia S., Abbate V., Meneghetti F., Frascione N., Hider R.C., Novellino E., Tron G.C., Giustiniano M.

Interrupted Ugi and Passerini Reactions: An Underexplored Treasure Island

Synthesis 2018, 50, 3549-3570

Giustiniano M., Moni L., Sangaletti L., Pelliccia S., Basso A., Novellino E., Tron G.C.

Arynes and isocyanides: Two close-knit partners in multicomponent reactions

Drug Discovery Today: Technologies 2018, 29, 35-41

Serafini M., Pirali T.

Rational Discovery of (+)-(S)-Abscisic Acid as a Potential Antifungal Agent: a Repurposing Approach

Scientific Reports 2018, 8, 8565-

Khedr A.M., Massarotti A., Mohamed M.E.

Targeting transient receptor potential vanilloid 1 (TRPV1) channel softly: the discovery of Passerini adducts as a topical treatment for inflammatory skin disorders

J. Med. Chem. 2018, 61, 4436-4455

Serafini M., Griglio A., Aprile S., Seiti F., Travelli C., Pattarino F., Grosa G., Sorba G., Genazzani A.A., Gonzales-Rodriguez S., Butron L., Devesa I., Fernández-Carvajal A., Pirali T., Ferrer-Montiel A.

Crystal structure of a thermophilic O6-alkylguanine-DNA alkyltransferase-derived self-labeling protein-tag in covalent complex with a fluorescent probe

Biochem Biophys Res Commun 2018, 500, 698-703

Rossi F., Morrone C., Massarotti A., Ferraris D.M., Valenti A., Perugino G., Miggiano R.

Non-hydrolytic chemoselective cleavage of Ugi tertiary amides: a mild access to N-substituted α-amino acid amides

Tetrahedron Lett. 2018, 59, 1196-1199

Giustiniano M., Pelliccia S., Novellino E., Tron G.C.

A multicomponent approach in the discovery of indoleamine 2,3-dioxygenase 1 inhibitors: synthesis, biological investigation and docking studies

Bioorganic Med. Chem. Lett 2018, 28, 651-657

Griglio A., Torre E., Serafini M., Bianchi A., Schmid R., Coda Zabetta G., Massarotti A., Sorba G., Pirali T., Fallarini S.

The hitchhiker’s guide to the chemical-biological galaxy

Drug Discovery Today 2018, 23, 565-574

Opassi G., Gesù A., Massarotti A.

Preparation of capsaicinoid transient receptor potential vanilloid 1 (TRPV1) via Passerini multicomponent reaction and their pharmaceutical, veterinary and cosmetic compositions

PCT Int. Appl. 2018, WO 2018206, -

Devesa G.I., Genazzani A.A., Pirali T., Fernandez-Carvajal A., Ferrer-Montiel A.V.

Modulators of SOCE, compositions, and uses thereof

PCT Int. Appl. 2017, WO20172124, -

Pirali T., Genazzani A.A., Riva B.

The use of 2-hydroxymethyl benzoic acid as an effective water surrogate in the Passerini reaction: A straightforward access to α-hydroxyamides

Tetrahedron Lett. 2017, 58, 4786-4789

Serafini M., Griglio A., Oberto E., Pirali T., Tron G.C.

Amphoteric 2-(Sulfonylamino)Benzaldehydes, Secondary Amines and Isocyanides in the Multicomponent Synthesis of Elusive N-Alkyl-2,3-diaminoindoles

Tetrahedron Lett. 2017, 58, 4264-4268

Giustiniano M., Pelliccia S., Sangaletti L., Meneghetti F., Amato J., Novellino E., Tron G.C.

An aryne-based three-component access to α-aroylamino amides

Org. Biom. Chem. 2017, 15, 6604-6612

Serafini M., Griglio A., Viarengo S., Aprile S., Pirali T.

Identification of a Potent Phosphoinositide 3-Kinase Pan Inhibitor Displaying a Strategic Carboxylic Acid Group and Development of Its Prodrugs

ChemMedChem 2017, 12, 1542-1554

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.

TRPM8 receptor agonist compounds and uses thereof

PCT Int. Appl. 2017, WO20171256, -

Ferrer Montiel A.V., Fernandez Carvajal A., Belmonte M.C., Gallar M.J., De La Torre R., Genazzani A.A., Tron G.C., Mercalli V.

A Fast Route for the Synthesis of Tetrazolyl Oximes by a Novel Multicomponent Reaction between Z-Chlorooximes, Isocyanides and Trimethylsilyl Azide

Tetrahedron Lett. 2017, 58, 3549-3553

Giustiniano M., Pelliccia S., Muñoz-Garcia A.B., Pavone M., Pagano B., Galli U., Novellino E., Tron G.C.

Structural investigations on orotate phosphoribosyltransferase from Mycobacterium tuberculosis, a key enzyme of the de novo pyrimidine biosynthesis

Scientific Reports 2017, 7, 1180-

Donini S., Ferraris D.F., Miggiano R., Massarotti A., Rizzi M.

Identification of Novel Triazole-Based Nicotinamide Phosphoribosyltransferase (NAMPT) Inhibitors Endowed with Anti-Proliferative and Anti-Inflammatory Activity

J. Med. Chem. 2017, 60, 1768-1792

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.

N–N bond formation in Ugi processes: from nitric acid to libraries of nitramines

Chem. Commun. 2017, 53, 2118-2121

Mercalli V., Nyadanu A., Cordier M., Tron G.C., Grimaud L.,El Kaim L.

To each his own: isonitriles for all flavors. Functionalized isocyaides as valuable tools in organic synthesis

Chem. Soc. Rev. 2017, 46, 1295-1357

Giustiniano M., Basso A., Mercalli V., Massarotti A., Novellino E., Tron G.C., Zhu J.

Interdomain interactions rearrangements control the reaction steps of a thermostable dna alkyltransferase

Biochimica et Biophysica Acta 2017, 2, 86-96

Morrone C., Miggiano R., Serpe M., Massarotti A., Valenti A., del Monaco G., Rossi M., Rossi F., Rizzi M., Perugino G., Ciaramella M.

A Successful Replacement of Phenols with Isocyanides in the Bargellini Reaction: Synthesis of 3-Carboxamido-Isobutyric acids

J. Org. Chem. 2016, 81, 11467-11471

Giustiniano M., Pelliccia S., Galli U., Amato J., Travagin F., Novellino E., Tron G.C.

Structural Biology in Antiviral Drug Discovery

Curr. Op. Pharm. 2016, 30, 116-130

Bassetto M., Massarotti A., Coluccia A., Brancale A.

The Metal Face of Protein Tyrosine Phosphatase 1B

Coord. Chem. Rev. 2016, 327–328, 70-83

Bellomo E., Kshetrimayum Singh B., Massarotti A., Hogstrand C., Maret W.

In silico-driven multicomponent synthesis of 4,5- and 1,5-disustituted imidazoles as indoleamine 2,3-dioxygenase inhibitors

Med. Chem. Commun. 2016, 7, 409-419

Fallarini S., Massarotti A., Gesù A., Giovarruscio S., Coda Zabetta G., Bergo R., Giannelli B., Brunco A., Lombardi G., Sorba G., Pirali T.

The Guareschi Pyridine Scaffold as a Valuable Platform for the Identification of Selective PI3K Inhibitors

Molecules 2015, 20, 17275-17287

Galli U., Ciraolo E., Massarotti A., Margaria J.P., Sorba G., Hirsch E., Tron G.C.

Identification of a novel NAMPT inhibitor by combinatorial click chemistry and chemical refinement

Med. Chem. Commun. 2015, 6, 1891-1897

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

Exploiting the Electrophilic and Nucleophilic Dual Role of Nitrile Imines: One-Pot, Three-Component Synthesis of Furo[2,3-d]pyridazin-4(5H)-ones

Org. Lett. 2015, 17, 3964-3967

Giustiniano M., Mercalli V., Amato J., Novellino E., Tron G.C.

Crystal structure of human nicotinic acid phosphoribosyltransferase

FEBS Open Bio 2015, 5, 419-428

Marletta S.A., Massarotti A., Orsomando G., Magni G., Rizzi M., Garavaglia S.

Design, Synthesis and Biological Evaluation of Combretabenzodiazepines: a Novel Class of Antitubulin Agents

J. Med. Chem. 2015, 58, 1345-1357

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.

Synthesis of Heteroarylogous 1H-Indole-3-Carboxamidines Through a Three-Component Interrupted Ugi Reaction

SYNTHESIS 2015, 47, 489-496

La Spisa F., Meneghetti F., Pozzi B., Tron G.C.

Inhibitors of nicotinamide phosphoribosyltransferase, compositions, products and uses thereof

PCT Int. Appl. 2014, WO2014178001 (A1), -

Genazzani A.A., Tron G.C., Galli U., Travelli C., Cuzzocrea S., Grosa G., Sorba G., Canonico P.L.

Solution phase parallel synthesis of aryloxyimino amides via a novel multicomponent reaction among aromatic (Z)-chlorooximes, isocyanides and electron deficient phenols

ACS Comb. Sci. 2014, 16, 602-605

Mercalli V., Giustiniano M., Del Grosso E., Varese M., Cassese H., Massarotti A., Novellino E., Tron G.C.

Synthesis of Aminocarbonyl N-Acylhydrazones by a Three-Component Reaction of Isocyanides, Hydrazonoyl Chlorides, and Carboxylic Acids

Org. Lett. 2014, 16, 5332-5335

Giustiniano M., Meneghetti F., Mercalli V., Varese M., Giustiniano F., Novellino E., Tron G.C.

Are 1,4- and 1,5-disubstituted-1,2,3-triazoles good pharmacophoric groups?

ChemMedChem 2014, 9, 2497-2508

Massarotti A., Aprile S., Mercalli V., Del Grosso E., Grosa G., Sorba G., Tron G.C.

Reaction Between (Z)-Arylchlorooximes and alpha-Isocyanoacetamides: a Procedure For The Synthesis of Aryl-alpha-Ketoamide amides

J. Org. Chem. 2014, 79, 6006-6014

Giustiniano M., Mercalli V., Cassese H., Di Maro S., Galli U., Novellino E., Tron G.C.

Zinc Ions Modulate Protein Tyrosine Phosphatase 1B activity

Metallomics 2014, 6, 1229-1239

Bellomo E., Massarotti A., Hogstrand C., Maret W.

The Nef Reaction of Isocyanides

SYNTHESIS 2014, 46, 829-841

La Spisa F., Tron G.C., El Kaïm L.

ZINClick: a database of 16 million novel, patentable and readily synthesizable 1,4-disubstituted triazoles

J. Chem. Inf. Model 2014, 54, 396-406

Massarotti A., Brunco A., Sorba G., Tron G.C.

Small molecule inhibitors of West Nile virus

Antivir. Chem. Chemother. 2014, 23, 179-187

Elseginy S.A., Massarotti A., Nawwar G.A., Amin K.M., Brancale A.

Isocyanide-Mediated Multicomponent Synthesis of C-Oximinoamidines

Org. Lett. 2013, 15, 5902-5905

Mercalli V., Meneghetti F., Tron G.C.

Medicinal Chemistry of Nicotinamide Phosphoribosyltransferase (NAMPT) inhibitors

J. Med. Chem. 2013, 56, 6279-6296

Galli U., Travelli C., Massarotti A., Fakhfouri G., Rahimian R., Tron G.C., Genazzani A.A.

Off the beaten track: the use of secondary amines in the Ugi reaction

Eur. J. Org. Chem. 2013, 2013, 1849-1859

Tron G.C.

Computer-aided identification, design and synthesis of a novel series of compounds with selective antiviral activity against chikungunya virus

Antvir. Res. 2013, 98, 12-18

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.

A Concise Synthesis of Pyrazole Analogues of Combretastatin A1 as Potent Antitubulin Agents

ChemMedChem 2013, 8, 633-643

Zaninetti R., Cortese S.V., Aprile S., Massarotti A., Canonico P.L., Sorba G., Grosa G., Genazzani A.A., Pirali T.

Parallel synthesis of “click” chalcones as antitubulin agents

Med. Chem. 2013, 9, 510-516

Utsintong M., Massarotti A., Caldarelli A., Theeramunkong S.

Nicotinamide phosphoribosyltransferase (NAMPT) is over-expressed in melanoma lesions

Pigment Cell Melanoma Res 2013, 26, 144-146

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.

An efficient synthesis of symmetric and unsymmetric bis-(β-aminoamides) via Ugi multicomponent reaction

Org. Lett. 2012, 14, 6044-6047

La Spisa F., Feo A., Mossetti R., Tron G.C.

Identification of a sirtuin 3 inhibitor that displays selectivity over sirtuin 1 and 2

Eu. J. Med. Chem. 2012, 55, 58-66

Galli U., Mesenzani O., Coppo C., Sorba G., Canonico P.L., Tron G.C., Genazzani A.A.

Quinolin-4 (1h)-one derivatives as inhibitors of phosphatidylinositol 3-kinases

PCT Int. Appl. 2012, WO 2012073, -

Sorba G., Tron G.C., Galli U., Massarotti A., Hirsch E., Ciraolo E., Pirali T.

PI3K keeps the balance between metabolism and cancer

Adv. Biol. Reg. 2012, 52, 389-405

Braccini L., Ciraolo E., Martini M., Pirali T., Germena G., Rolfo K., Hirsch E.

Haptic-Driven applications to Molecular Modelling: State of the Art and Perspectives

Future Med. Chem. 2012, 4, 1219-1228

Ricci A., Anthopoulos A., Massarotti A., Grimstead I., Brancale A.

The NAMPT inhibitor FK866 reverts the damage in spinal cord injury

J. Neuroinflammation 2012, 9, 66-77

Esposito E., Impellizzeri D., Mazzon E., Fakhfouri G., Rahimian R., Travelli C., Tron G.C., Genazzani A.A., Cuzzocrea S.

De novo computer-aided design of novel antiviral agents

Drug Discovery Today: Technologies 2012, 9, e213-e218

Massarotti A., Coluccia A., Sorba G., Silvestri R., Brancale A.

Transition metal-free direct arylation of anilines

Angew. Chem. Int. Ed. 2012, 51, 1006-1009

Pirali T., Zhang F., Miller A.H., Head J.L., McAusland D., Greaney M.F.

The tubulin colchicine domain: a molecular modelling perspective

ChemMedChem 2012, 7, 33-42

Massarotti A., Coluccia A., Silvestri R., Sorba G., Brancale A.

Identification of novel antitubulin agents by using a virtual screening approach based on a 7-point pharmacophore model of the tubulin Colchi-site

Chem. Biol. Drug Des. 2011, 78, 913-922

Massarotti A., Theeramunkong S., Mesenzani O., Caldarelli A., Genazzani A.A., Tron G.C.

Pietro Biginelli: The Man Behind the Reaction

Eur. J. Org. Chem. 2011, 2011, 5541-5550

Tron G.C., Minassi A., Appendino G.

Regioselective Suzuki coupling of dihaloheteroaromatic compounds as a rapid strategy to synthesize potent rigid combretastatin analogues

J. Med. Chem. 2011, 54, 4977-4986

Theeramunkong S., Caldarelli A., Massarotti A., Aprile S., Caprioglio D., Zaninetti R., Teruggi A., Pirali T., Grosa G., Tron G.C., Genazzani A.A.

Reciprocal potentiation of the antitumoral activities of FK866, an inhibitor of nicotinamide phosphoribosyltransferase, and etoposide or cisplatin in neuroblastoma cells

J. Pharm. Exp. Therap. 2011, 338, 829-840

Travelli C., Drago V., Maldi E., Kaludercic N., Galli U., Boldorini R., Di Lisa F., Tron G.C., Canonico P.L., Genazzani A.A.

Imides: Forgotten Players in the Ugi reaction. One pot multicomponent synthesis of quinazolinones

Chem. Comm. 2011, 47, 6966-6968

Mossetti R., Pirali T., Saggiorato D., Tron G.C.

Groebke multicomponent reaction and subsequent nucleophilic aromatic substitution for a convenient synthesis of 3,8-diaminoimidazo[1,2-a]pyrazines as potential kinase inhibitors

Org. Biomol. Chem. 2011, 9, 4144-4149

Guasconi M., Lu X., Massarotti A., Caldarelli A., Ciraolo E., Tron G.C., Hirsch E., Sorba G., Pirali T.

A novel a-isocyanoacetamide-based three-component reaction for the synthesis of dialkyl 2-acyl-5-aminofuran-3,4-dicarboxylates

Org. Biomol. Chem. 2011, 9, 1627-1631

Mossetti R., Caprioglio D., Colombano G., Tron G.C., Pirali T.

Replacement of the double bond of antitubulin chalcones with triazoles and tetrazoles: synthesis and biological evaluation

Bioorg. Med. Chem. Lett. 2011, 21, 764-768

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.

A Practical Synthesis of 5-Aroyl-1-aryltetrazoles Using an Ugi-Like 4-Component Reaction Followed by a Biomimetic Transamination

Synthesis 2010, 23, 4107-4118

Giustiniano M., Pirali T., Massarotti A., Biletta B., Novellino E., Campiglia P., Sorba G., Tron G.C.

Essential role of the p110beta subunit of phosphoinositide 3-OH kinase in male fertility

Mol. Biol. Cell. 2010, 21, 704-711

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.

Stereoselective synthesis of trans-beta-lactams by palladium-catalysed carbonylation of vinyl aziridines

Chem. Commun. 2010, 46, 267-269

Fontana F., Tron G.C., Barbero N., Ferrini S., Thomas S.P., Aggarwal V.K.

A novel potent nicotinamide phosphoribosyltransferase inhibitor synthesized via click chemistry

J. Med. Chem. 2010, 53, 616-623

Colombano G., Travelli T., Galli U., Caldarelli A., Chini M.G., Canonico P.L., Sorba G., Bifulco G., Tron G.C., Genazzani A.A.

Synthesis, molecular docking and biological evaluation as HDAC inhibitors of cyclopeptide mimetics by a tandem three-component reaction and intramolecular [3+2] cycloaddition

Mol. Divers. 2010, 14, 109-121

Pirali T., Faccio V., Mossetti R., Grolla A.A., Di Micco S., Bifulco G., Genazzani A.A., Tron G.C.

Synthesis of Passerini-Ugi Hybrids by a Four-Component Reaction Using the Glycolaldehyde Dimer

J. Org. Chem. 2009, 74, 4890-4892

Mossetti R., Pirali T., Tron G.C.

Synthesis, biological evaluation, and molecular docking of Ugi products containing a zinc-chelating moiety as novel inhibitors of histone deacetylases

J. Med. Chem. 2009, 52, 2776-2785

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.

A coincise entry into non-symmetrical alkyl polyamines

Org. Lett. 2008, 10, 4199-4202

Pirali T., Callipari G., Ercolano E., Genazzani A.A., Giovenzana G.B., Tron G.C.

Characterization of NAD uptake in mammalian cells

J. Biol. Chem. 2008, 283, 6367-6374

Billington R.A., Travelli C., Ercolano E., Galli U., Roman C., Grolla A.A., Canonico P.L., Condorelli F., Genazzani A.A.

Solution-phase parallel synthesis and biological evaluation of combretatriazoles

J. Comb. Chem. 2008, 10, 732-740

Cafici L., Pirali T., Condorelli F., Del Grosso E., Massarotti A., Sorba G., Canonico P.L., Tron G.C., Genazzani A.A.

Triazole-modified histone deacetylase inhibitors as a rapid route to drug discovery

J. Comb. Chem. 2008, 10, 624-627

Pirali T., Pagliai F., Mercurio C., Boggio R., Canonico P.L., Sorba G., Tron G.C., Genazzani A.A.

Synthesis and biological evaluation of isosteric analogues of FK866, an inhibitor of NAD salvage

ChemMedChem 2008, 3, 771-779

Galli U., Ercolano E., Carraro L., Blasi Roman C.R., Sorba G., Canonico P.L., Genazzani A.A., Tron G.C., Billington R.A.

Click chemistry reactions in medicinal chemistry: applications of the 1,3-dipolar cycloaddition between azides and alkynes

Med. Res. Rev. 2008, 28, 278-308

Tron G.C., Pirali T., Billington R., Canonico P.L., Sorba G., Genazzani A.

In vitro metabolism study of combretastatin A-4 in rat and human liver microsome

Drug Metab. Dispo. 2007, 35, 2252-2261

Aprile S., Del Grosso E., Tron G.C., Grosa G.

Replacement of the lactone moiety on podophyllotoxin and steganacin analogues with a 1,5-disubstituted 1,2,3-triazole via ruthenium-catalyzed click chemistry

Bioorg. Med. Chem. 2007, 15, 6748-6757

Imperio D., Pirali T., Galli U., Pagliai F., Cafici L., Canonico P.L., Sorba G., Genazzani A.A., Tron G.C.

Estrogenic analogues synthesized via click chemistry

ChemMedChem 2007, 2, 437-440

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.

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

Bioorg. Med. Chem. Lett. 2007, 17, 220-224

Galli U., Oliaro-Bosso S., Taramino S., Venegoni S., Pastore E., Tron G.C., Balliano G., Viola F., Sorba G.

Synthesis and cytotoxic evaluation of combretafurans, potential scaffolds for dual-action antitumoral agents

J. Med. Chem. 2006, 49, 5372-5376

Pirali T., Busacca S., Beltrami L., Imovilli D., Pagliai F., Miglio G., Massarotti A., Verotta L., Tron G.C., Sorba G., Genazzani A.A.

Medicinal chemistry of combretastatin A-4: present and future directions

J. Med. Chem. 2006, 49, 3033-3044

Tron G.C., Pirali T., Sorba G., Pagliai F., Busacca S., Genazzani A.A.

Split the primary amine in two: secondary diamines may play the role of the primary amine in the Ugi 4CR

Angew. Chem. Int. Ed. 2006, 45, 1099-1102

Giovenzana G.B., Tron G.C., Di Paola S., Menegotto I.G., Pirali T.

Rapid synthesis of triazole-modified resveratrol analogues via click chemistry

J. Med. Chem. 2006, 49, 467-470

Pagliai F., Pirali T., Del Grosso E., Di Brisco R., Tron G.C., Sorba G., Genazzani A.A.

Synthesis and biological activity of mustard derivatives of combretastatins

Bioorg. Med. Chem. Lett. 2005, 15, 3551-3554

Coggiola B., Pagliai F., Allegrone G., Genazzani A.A., Tron G.C.

Synthesis and cytotoxic evaluation of combretafurazans

J. Med. Chem. 2005, 48, 3260-3268

Tron G.C., Pagliai F., Del Grosso E., Genazzani A.A., Sorba G.

Role of the nicotinic acid group in NAADP receptor selectivity

Cell Calcium 2005, 37, 81-86

Billington R.A., Tron G.C., Reichenbach S., Sorba G., Genazzani A.A.