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Items: 40

1.

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

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

Dis Model Mech. 2019 Dec 3;13(2). pii: dmm041111. doi: 10.1242/dmm.041111.

2.

A primer of deuterium in drug design.

Cargnin S, Serafini M, Pirali T.

Future Med Chem. 2019 Aug;11(16):2039-2042. doi: 10.4155/fmc-2019-0183. No abstract available.

3.

Soft drugs for dermatological applications: recent trends.

Aprile S, Serafini M, Pirali T.

Drug Discov Today. 2019 Dec;24(12):2234-2246. doi: 10.1016/j.drudis.2019.08.007. Epub 2019 Sep 5. Review.

PMID:
31494188
4.

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

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

Molecules. 2019 May 15;24(10). pii: E1874. doi: 10.3390/molecules24101874.

5.

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

Pirali T, Galli U, Serafini M, Griglio A, Genazzani AA, Tron GC.

Methods Mol Biol. 2019;1987:207-221. doi: 10.1007/978-1-4939-9446-5_13.

PMID:
31028682
6.

Applications of Deuterium in Medicinal Chemistry.

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

J Med Chem. 2019 Jun 13;62(11):5276-5297. doi: 10.1021/acs.jmedchem.8b01808. Epub 2019 Jan 25.

PMID:
30640460
7.

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

Campa CC, Silva RL, Margaria JP, Pirali T, Mattos MS, Kraemer LR, Reis DC, Grosa G, Copperi F, Dalmarco EM, Lima-Júnior RCP, Aprile S, Sala V, Dal Bello F, Prado DS, Alves-Filho JC, Medana C, Cassali GD, Tron GC, Teixeira MM, Ciraolo E, Russo RC, Hirsch E.

Nat Commun. 2018 Dec 12;9(1):5232. doi: 10.1038/s41467-018-07698-6.

8.

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

Serafini M, Pirali T.

Drug Discov Today Technol. 2018 Nov;29:35-41. doi: 10.1016/j.ddtec.2018.06.007. Epub 2018 Jul 2. Review.

PMID:
30471672
9.

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

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 PL, Cuzzocrea S, Genazzani AA, Pirali T.

J Med Chem. 2018 Nov 8;61(21):9756-9783. doi: 10.1021/acs.jmedchem.8b01512. Epub 2018 Oct 30.

PMID:
30347159
10.

Targeting Transient Receptor Potential Vanilloid 1 (TRPV1) Channel Softly: The Discovery of Passerini Adducts as a Topical Treatment for Inflammatory Skin Disorders.

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

J Med Chem. 2018 May 24;61(10):4436-4455. doi: 10.1021/acs.jmedchem.8b00109. Epub 2018 May 15.

PMID:
29722529
11.

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

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

Bioorg Med Chem Lett. 2018 Feb 15;28(4):651-657. doi: 10.1016/j.bmcl.2018.01.032. Epub 2018 Feb 2.

PMID:
29398544
12.

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, Campa CC, Margaria JP, Silva RL, Grosa G, Sorba G, Williams R, Hirsch E, Tron GC.

ChemMedChem. 2017 Sep 21;12(18):1542-1554. doi: 10.1002/cmdc.201700340. Epub 2017 Aug 31.

13.

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

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

Org Biomol Chem. 2017 Aug 9;15(31):6604-6612. doi: 10.1039/c7ob01715d.

PMID:
28752162
14.

Transition-Metal-Free Synthesis of 2-Arylimidazolones via Cascade Reaction between Arynes and α,α'-Disubstituted α-Isocyanoacetamides.

Gesù A, Pozzoli C, Torre E, Aprile S, Pirali T.

Org Lett. 2016 May 6;18(9):1992-5. doi: 10.1021/acs.orglett.6b00580. Epub 2016 Apr 8.

PMID:
27057924
15.

A concise synthesis of pyrazole analogues of combretastatin A1 as potent anti-tubulin agents.

Zaninetti R, Cortese SV, Aprile S, Massarotti A, Canonico PL, Sorba G, Grosa G, Genazzani AA, Pirali T.

ChemMedChem. 2013 Apr;8(4):633-43. doi: 10.1002/cmdc.201200561. Epub 2013 Feb 21.

PMID:
23436706
16.

PI3K keeps the balance between metabolism and cancer.

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

Adv Biol Regul. 2012 Sep;52(3):389-405. doi: 10.1016/j.jbior.2012.04.002. Epub 2012 Apr 24. Review.

PMID:
22884032
17.

Transition-metal-free direct arylation of anilines.

Pirali T, Zhang F, Miller AH, Head JL, McAusland D, Greaney MF.

Angew Chem Int Ed Engl. 2012 Jan 23;51(4):1006-9. doi: 10.1002/anie.201106150. Epub 2011 Dec 12. No abstract available.

PMID:
22162111
18.

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 GC, Genazzani AA.

J Med Chem. 2011 Jul 28;54(14):4977-86. doi: 10.1021/jm200555r. Epub 2011 Jun 30.

PMID:
21696175
19.

Stereospecific synthesis of syn-α-oximinoamides by a three-component reaction of isocyanides, syn-chlorooximes, and carboxylic acids.

Pirali T, Mossetti R, Galli S, Tron GC.

Org Lett. 2011 Jul 15;13(14):3734-7. doi: 10.1021/ol201397x. Epub 2011 Jun 13.

PMID:
21667987
20.

Imides: forgotten players in the Ugi reaction. One-pot multicomponent synthesis of quinazolinones.

Mossetti R, Pirali T, Saggiorato D, Tron GC.

Chem Commun (Camb). 2011 Jun 28;47(24):6966-8. doi: 10.1039/c1cc12067k. Epub 2011 May 17.

PMID:
21589958
21.

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 GC, Hirsch E, Sorba G, Pirali T.

Org Biomol Chem. 2011 Jun 7;9(11):4144-9. doi: 10.1039/c1ob05336a. Epub 2011 Apr 14.

PMID:
21494711
22.

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

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

Org Biomol Chem. 2011 Mar 7;9(5):1627-31. doi: 10.1039/c0ob00979b. Epub 2011 Jan 20.

PMID:
21249262
23.

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, Sorba G, Novellino E, Genazzani AA, Tron GC.

Bioorg Med Chem Lett. 2011 Jan 15;21(2):764-8. doi: 10.1016/j.bmcl.2010.11.113. Epub 2010 Nov 28.

PMID:
21167709
24.

Activation of TRPV4 channels reduces migration of immortalized neuroendocrine cells.

Zaninetti R, Fornarelli A, Ciarletta M, Lim D, Caldarelli A, Pirali T, Cariboni A, Owsianik G, Nilius B, Canonico PL, Distasi C, Genazzani AA.

J Neurochem. 2011 Feb;116(4):606-15. doi: 10.1111/j.1471-4159.2010.07144.x. Epub 2011 Jan 19.

25.

Efficient synthesis of alpha-ketoamides via 2-acyl-5-aminooxazoles by reacting acyl chlorides and alpha-isocyanoacetamides.

Mossetti R, Pirali T, Tron GC, Zhu J.

Org Lett. 2010 Feb 19;12(4):820-3. doi: 10.1021/ol902894p.

PMID:
20088495
26.

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 AA, Di Micco S, Bifulco G, Genazzani AA, Tron GC.

Mol Divers. 2010 Feb;14(1):109-21. doi: 10.1007/s11030-009-9153-9. Epub 2009 May 28.

PMID:
19475493
27.

Synthesis of Passerini-Ugi hybrids by a four-component reaction using the glycolaldehyde dimer.

Mossetti R, Pirali T, Tron GC.

J Org Chem. 2009 Jul 3;74(13):4890-2. doi: 10.1021/jo9005969.

PMID:
19449841
28.

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

Grolla AA, Podestà V, Chini MG, Di Micco S, Vallario A, Genazzani AA, Canonico PL, Bifulco G, Tron GC, Sorba G, Pirali T.

J Med Chem. 2009 May 14;52(9):2776-85. doi: 10.1021/jm801529c.

PMID:
19344175
29.

A concise entry into nonsymmetrical alkyl polyamines.

Pirali T, Callipari G, Ercolano E, Genazzani AA, Giovenzana GB, Tron GC.

Org Lett. 2008 Oct 2;10(19):4199-202. doi: 10.1021/ol801612r. Epub 2008 Sep 3.

PMID:
18763798
30.

Solution-phase parallel synthesis and biological evaluation of combretatriazoles.

Cafici L, Pirali T, Condorelli F, Del Grosso E, Massarotti A, Sorba G, Canonico PL, Tron GC, Genazzani AA.

J Comb Chem. 2008 Sep-Oct;10(5):732-40. doi: 10.1021/cc800090d. Epub 2008 Aug 6.

PMID:
18681482
31.

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

Pirali T, Pagliai F, Mercurio C, Boggio R, Canonico PL, Sorba G, Tron GC, Genazzani AA.

J Comb Chem. 2008 Sep-Oct;10(5):624-7. doi: 10.1021/cc800061c. Epub 2008 Jul 4. No abstract available.

PMID:
18598089
32.

Ammonium chloride promoted three-component synthesis of 5-iminooxazoline and its subsequent transformation to macrocyclodepsipeptide.

Pirali T, Tron GC, Masson G, Zhu J.

Org Lett. 2007 Dec 6;9(25):5275-8. Epub 2007 Nov 9.

PMID:
17990892
33.

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 PL, Sorba G, Genazzani AA, Tron GC.

Bioorg Med Chem. 2007 Nov 1;15(21):6748-57. Epub 2007 Aug 22.

PMID:
17765552
34.

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

Tron GC, Pirali T, Billington RA, Canonico PL, Sorba G, Genazzani AA.

Med Res Rev. 2008 Mar;28(2):278-308. Review.

PMID:
17763363
35.

Estrogenic analogues synthesized by click chemistry.

Pirali T, Gatti S, Di Brisco R, Tacchi S, Zaninetti R, Brunelli E, Massarotti A, Sorba G, Canonico PL, Moro L, Genazzani AA, Tron GC, Billington RA.

ChemMedChem. 2007 Apr;2(4):437-40. No abstract available.

PMID:
17278167
36.
37.

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 GC, Sorba G, Genazzani AA.

J Med Chem. 2006 Aug 24;49(17):5372-6.

PMID:
16913727
38.

Medicinal chemistry of combretastatin A4: present and future directions.

Tron GC, Pirali T, Sorba G, Pagliai F, Busacca S, Genazzani AA.

J Med Chem. 2006 Jun 1;49(11):3033-44. Review. No abstract available.

PMID:
16722619
39.

Rapid synthesis of triazole-modified resveratrol analogues via click chemistry.

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

J Med Chem. 2006 Jan 26;49(2):467-70.

PMID:
16420033
40.

A mimicry of primary amines by bis-secondary diamines as components in the Ugi four-component reaction.

Giovenzana GB, Tron GC, Di Paola S, Menegotto IG, Pirali T.

Angew Chem Int Ed Engl. 2006 Feb 6;45(7):1099-102. No abstract available.

PMID:
16389629

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