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Items: 1 to 50 of 57

1.

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

Travelli C, Aprile S, Mattoteia D, Colombo G, Clemente N, Scanziani E, Terrazzino S, Alisi MA, Polenzani L, Grosa G, Genazzani AA, Tron GC, Galli U.

Eur J Med Chem. 2019 Nov 1;181:111576. doi: 10.1016/j.ejmech.2019.111576. Epub 2019 Aug 1.

PMID:
31400709
2.

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-JĂșnior 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.

3.

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
4.

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
5.

Troxerutin, a mixture of O-hydroxyethyl derivatives of the natural flavonoid rutin: Chemical stability and analytical aspects.

Bianchi M, Canavesi R, Aprile S, Grosa G, Del Grosso E.

J Pharm Biomed Anal. 2018 Feb 20;150:248-257. doi: 10.1016/j.jpba.2017.12.018. Epub 2017 Dec 9.

PMID:
29258044
6.

Biological effects of combined resveratrol and vitamin D3 on ovarian tissue.

Uberti F, Morsanuto V, Aprile S, Ghirlanda S, Stoppa I, Cochis A, Grosa G, Rimondini L, Molinari C.

J Ovarian Res. 2017 Sep 15;10(1):61. doi: 10.1186/s13048-017-0357-9.

7.

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.

8.

New insights in the metabolism of oxybutynin: evidence of N-oxidation of propargylamine moiety and rearrangement to enaminoketone.

Aprile S, Canavesi R, Matucci R, Bellucci C, Del Grosso E, Grosa G.

Xenobiotica. 2018 May;48(5):478-487. doi: 10.1080/00498254.2017.1342288. Epub 2017 Jul 6.

PMID:
28608746
9.

Identification of Novel Triazole-Based Nicotinamide Phosphoribosyltransferase (NAMPT) Inhibitors Endowed with Antiproliferative and Antiinflammatory Activity.

Travelli C, Aprile S, Rahimian R, Grolla AA, 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, Troiani MP, Alisi MA, Grosa G, Sorba G, Canonico PL, Orsomando G, Cuzzocrea S, Genazzani AA, Galli U, Tron GC.

J Med Chem. 2017 Mar 9;60(5):1768-1792. doi: 10.1021/acs.jmedchem.6b01392. Epub 2017 Feb 22.

PMID:
28165742
10.

Development and validation of a stability-indicating HPLC-UV method for the determination of Thiocolchicoside and its degradation products.

Aprile S, Canavesi R, Bianchi M, Grosa G, Del Grosso E.

J Pharm Biomed Anal. 2017 Jan 5;132:66-71. doi: 10.1016/j.jpba.2016.09.037. Epub 2016 Sep 26.

PMID:
27697571
11.

New insights in oxybutynin chemical stability: Identification in transdermal patches of a new impurity arising from oxybutynin N-oxide rearrangement.

Canavesi R, Aprile S, Giovenzana GB, Di Sotto A, Di Giacomo S, Del Grosso E, Grosa G.

Eur J Pharm Sci. 2016 Mar 10;84:123-31. doi: 10.1016/j.ejps.2016.01.015. Epub 2016 Jan 18.

PMID:
26796144
12.

Design, synthesis, and biological evaluation of combretabenzodiazepines: a novel class of anti-tubulin agents.

Galli U, Travelli C, Aprile S, Arrigoni E, Torretta S, Grosa G, Massarotti A, Sorba G, Canonico PL, Genazzani AA, Tron GC.

J Med Chem. 2015 Feb 12;58(3):1345-57. doi: 10.1021/jm5016389. Epub 2015 Jan 27.

PMID:
25584687
13.

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 GC.

ChemMedChem. 2014 Nov;9(11):2497-508. doi: 10.1002/cmdc.201402233. Epub 2014 Jul 30.

PMID:
25079879
14.

Development and validation of a stability-indicating LC-UV method for the determination of pantethine and its degradation product based on a forced degradation study.

Canavesi R, Aprile S, Varese E, Grosa G.

J Pharm Biomed Anal. 2014 Aug;97:141-50. doi: 10.1016/j.jpba.2014.04.025. Epub 2014 May 2.

PMID:
24863372
15.

Metabolic fate of combretastatin A-1: LC-DAD-MS/MS investigation and biological evaluation of its reactive metabolites.

Aprile S, Zaninetti R, Del Grosso E, Genazzani AA, Grosa G.

J Pharm Biomed Anal. 2013 May 5;78-79:233-42. doi: 10.1016/j.jpba.2013.02.030. Epub 2013 Feb 27.

PMID:
23501444
16.

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
17.

In vitro metabolic fate of alizapride: evidence for the formation of reactive metabolites based on liquid chromatography-tandem mass spectrometry.

Aprile S, Del Grosso E, Grosa G.

J Mass Spectrom. 2012 Jun;47(6):737-50. doi: 10.1002/jms.3011.

PMID:
22707166
18.

The metabolic fate of isocombretastatin A-4 in human liver microsomes: identification, synthesis and biological evaluation of metabolites.

Soussi MA, Aprile S, Messaoudi S, Provot O, Del Grosso E, Bignon J, Dubois J, Brion JD, Grosa G, Alami M.

ChemMedChem. 2011 Oct 4;6(10):1781-8. doi: 10.1002/cmdc.201100193. Epub 2011 Jul 11. No abstract available.

PMID:
21748852
19.

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
20.

In vitro metabolism study of 2-isopropyl-9H-thioxanthen-9-one (2-ITX) in rat and human: evidence for the formation of an epoxide metabolite.

Aprile S, Del Grosso E, Grosa G.

Xenobiotica. 2011 Mar;41(3):212-25. doi: 10.3109/00498254.2010.532887. Epub 2010 Nov 18.

PMID:
21087117
21.

Identification of the human UDP-glucuronosyltransferases involved in the glucuronidation of combretastatin A-4.

Aprile S, Del Grosso E, Grosa G.

Drug Metab Dispos. 2010 Jul;38(7):1141-6. doi: 10.1124/dmd.109.031435. Epub 2010 Apr 7.

PMID:
20375181
22.

Development and validation of a stability-indicating HPLC-UV method for the determination of alizapride and its degradation products.

Tamaro I, Aprile S, Giovenzana GB, Grosa G.

J Pharm Biomed Anal. 2010 Apr 6;51(5):1024-31. doi: 10.1016/j.jpba.2009.10.026. Epub 2009 Nov 6.

PMID:
19962264
23.

Realization of the compact static Fourier transform spectrometer LLIFTS in glass integrated optics.

Martin B, Morand A, Benech P, Grosa G, Kern P, Jocou L, Le Coarer E.

Opt Lett. 2009 Aug 1;34(15):2291-3.

PMID:
19649074
24.

Lack of in vitro interactions using human liver microsomes between rabeprazole and anticancer drugs.

Tamaro I, Genazzani A, Canonico P, Grosa G.

Eur J Drug Metab Pharmacokinet. 2009 Jan-Mar;34(1):19-26.

PMID:
19462924
25.

In vitro and in vivo phase II metabolism of combretastatin A-4: evidence for the formation of a sulphate conjugate metabolite.

Aprile S, Del Grosso E, Grosa G.

Xenobiotica. 2009 Feb;39(2):148-61. doi: 10.1080/00498250802566976.

PMID:
19255941
26.

Development and validation of a solid-phase extraction and gas chromatography-tandem mass spectrometry method for the determination of isopropyl-9H-thioxanthen-9-one in carton packaged milk.

Allegrone G, Tamaro I, Spinardi S, Grosa G.

J Chromatogr A. 2008 Dec 19;1214(1-2):128-33. doi: 10.1016/j.chroma.2008.10.019. Epub 2008 Oct 14.

PMID:
18992884
27.

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

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

Drug Metab Dispos. 2007 Dec;35(12):2252-61. Epub 2007 Sep 21.

PMID:
17890446
28.

Simultaneous, stability indicating, HPLC-DAD determination of guaifenesin and methyl and propyl-parabens in cough syrup.

Grosa G, Del Grosso E, Russo R, Allegrone G.

J Pharm Biomed Anal. 2006 Jun 7;41(3):798-803. Epub 2006 Feb 23.

PMID:
16497471
29.

LC-ESI-MS/MS characterization of strophanthin-K.

Grosa G, Allegrone G, Del Grosso E.

J Pharm Biomed Anal. 2005 Jun 1;38(1):79-86. Epub 2005 Jan 19.

PMID:
15907623
30.

Identification of 2,3-diaminophenazine and of o-benzoquinone dioxime as the major in vitro metabolites of benzofuroxan.

Grosa G, Galli U, Rolando B, Fruttero R, Gervasio G, Gasco A.

Xenobiotica. 2004 Apr;34(4):345-52.

PMID:
15268979
31.

Thiol-modifying inhibitors for understanding squalene cyclase function.

Milla P, Lenhart A, Grosa G, Viola F, Weihofen WA, Schulz GE, Balliano G.

Eur J Biochem. 2002 Apr;269(8):2108-16.

32.

Nitroanilines are the reduction products of benzofuroxan system by oxyhemoglobin (HbO2 2+).

Medana C, Visentin S, Grosa G, Fruttero R, Gasco A.

Farmaco. 2001 Oct;56(10):799-802.

PMID:
11718274
33.

2,3-Oxidosqualene cyclase: from azasqualenes to new site-directed inhibitors.

Cattel L, Ceruti M, Balliano G, Viola F, Grosa G, Rocco F, Brusa P.

Lipids. 1995 Mar;30(3):235-46.

PMID:
7791532
34.

Solubilization and identification of essential functional groups of Candida albicans oxidosqualene cyclase.

Carrano L, Noe M, Grosa G, Milla P, Denaro M, Islam K.

J Med Vet Mycol. 1995 Jan-Feb;33(1):53-8.

PMID:
7650579
35.

Metabolism of 4-(3-cyclohexylpropionyl)-1-(2-ethoxyphenyl) piperazine (D-16120) by rat liver microsomes.

Caputo O, Rocco F, Grosa G.

Eur J Drug Metab Pharmacokinet. 1994 Oct-Dec;19(4):303-10.

PMID:
7737231
36.

2,3,4,5-tetrahydroxy-5-(4-hydroxyphenyl)valeric acid: a new cleavable monofunctional reagent for monoclonal antibody labeling.

Grosa G, Dosio F, Brusa P, Ceruti M, Delprino L, Cattel L.

Farmaco. 1994 May;49(5):349-55.

PMID:
8080618
37.

Pharmacokinetics of an antibody-ricin conjugate administered intraperitoneally to mice.

Brusa P, Dosio F, Pacchioni D, Delprino L, Grosa G, Bussolati G, Cattel L.

J Pharm Sci. 1994 Apr;83(4):514-9.

PMID:
8046606
38.

A new approach in the synthesis of immunotoxins: ribosome inactivating protein noncovalently bound to monoclonal antibody.

Dosio F, Brusa P, Delprino L, Grosa G, Ceruti M, Cattel L.

J Pharm Sci. 1994 Feb;83(2):206-11.

PMID:
8169790
39.

3-Carboxy-4-nitrophenyl-dithio-1,1',2-trisnorsqualene: a site-directed inactivator of yeast oxidosqualene cyclase.

Balliano G, Grosa G, Milla P, Viola F, Cattel L.

Lipids. 1993 Oct;28(10):903-6.

PMID:
8246689
40.

Toxin-targeted design for anticancer therapy. II: Preparation and biological comparison of different chemically linked gelonin-antibody conjugates.

Delprino L, Giacomotti M, Dosio F, Brusa P, Ceruti M, Grosa G, Cattel L.

J Pharm Sci. 1993 Jul;82(7):699-704.

PMID:
8360843
41.

Toxin-targeted design for anticancer therapy. I: Synthesis and biological evaluation of new thioimidate heterobifunctional reagents.

Delprino L, Giacomotti M, Dosio F, Brusa P, Ceruti M, Grosa G, Cattel L.

J Pharm Sci. 1993 May;82(5):506-12.

PMID:
8360828
42.
43.

A new 'solid phase' procedure to synthesize immunotoxins (antibody-ribosome inactivating protein conjugates).

Dosio F, Brusa P, Delprino L, Ceruti M, Grosa G, Cattel L, Bolognesi A, Barbieri L.

Farmaco. 1993 Jan;48(1):105-15.

PMID:
8457275
44.
45.

2,3-Epoxy-10-aza-10,11-dihydrosqualene, a high-energy intermediate analogue inhibitor of 2,3-oxidosqualene cyclase.

Ceruti M, Balliano G, Viola F, Grosa G, Rocco F, Cattel L.

J Med Chem. 1992 Aug 7;35(16):3050-8.

PMID:
1501233
46.

The metabolic fate of the anti-parkinsonian drug budipine in rats.

Caputo O, Grosa G, Ceruti M, Rocco F, Biglino G.

Eur J Drug Metab Pharmacokinet. 1991 Apr-Jun;16(2):113-8.

PMID:
1936070
47.

Metabolism of 7-(1,3-dithiolan-2-ylmethyl)-1,3-dimethylxanthine by rat liver microsomes. Diastereoselective metabolism of the 1,3-dithiolane ring.

Grosa G, Caputo O, Ceruti M, Biglino G, Franzone JS, Cravanzola C.

Drug Metab Dispos. 1991 Mar-Apr;19(2):454-7.

PMID:
1676653
48.

Metabolism of 1,1-dichloro-cis-diphenylcyclopropane by rat liver microsomes.

Caputo O, Grosa G, Ceruti M, Rocco F, Biglino G.

Drug Metab Dispos. 1990 Sep-Oct;18(5):771-8.

PMID:
1981735
49.

Kinetic and metabolic studies of 7-(1,3-dithiolan-2-ylmethyl)-1,3-dimethylxanthine in the rat.

Cravanzola C, Grosa G, Franzone JS.

Drugs Exp Clin Res. 1990;16(6):285-91.

PMID:
2086163
50.

In vivo metabolism of the anti-inflammatory agent 2-(5-ethylpyridin-2-yl)benzimidazole.

Caputo O, Grosa G, Ceruti M, Viola F, Rocco F.

Eur J Drug Metab Pharmacokinet. 1989 Oct-Dec;14(4):263-8.

PMID:
2633920

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