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Items: 38

1.

Tranylcypromine-Based LSD1 Inhibitors: Structure-Activity Relationships, Antiproliferative Effects in Leukemia, and Gene Target Modulation.

Fioravanti R, Romanelli A, Mautone N, Di Bello E, Rovere A, Corinti D, Zwergel C, Valente S, Rotili D, Botrugno OA, Dessanti P, Vultaggio S, Vianello P, Cappa A, Binda C, Mattevi A, Minucci S, Mercurio C, Varasi M, Mai A.

ChemMedChem. 2020 Jan 31. doi: 10.1002/cmdc.201900730. [Epub ahead of print]

PMID:
32003940
2.

Amyloid Cardiomyopathy in the Rare Transthyretin Tyr78Phe Mutation.

Tini G, Vianello PF, Gemelli C, Grandis M, Canepa M.

J Cardiovasc Transl Res. 2019 Dec;12(6):514-516. doi: 10.1007/s12265-018-9859-0. Epub 2019 Jan 2.

PMID:
30604309
3.

Novel potent inhibitors of the histone demethylase KDM1A (LSD1), orally active in a murine promyelocitic leukemia model.

Trifirò P, Cappa A, Brambillasca S, Botrugno OA, Cera MR, Zuffo RD, Dessanti P, Meroni G, Thaler F, Villa M, Minucci S, Mercurio C, Varasi M, Vianello P.

Future Med Chem. 2017 Jul;9(11):1161-1174. doi: 10.4155/fmc-2017-0003. Epub 2017 Jul 19.

PMID:
28722470
4.

Thieno[3,2-b]pyrrole-5-carboxamides as New Reversible Inhibitors of Histone Lysine Demethylase KDM1A/LSD1. Part 2: Structure-Based Drug Design and Structure-Activity Relationship.

Vianello P, Sartori L, Amigoni F, Cappa A, Fagá G, Fattori R, Legnaghi E, Ciossani G, Mattevi A, Meroni G, Moretti L, Cecatiello V, Pasqualato S, Romussi A, Thaler F, Trifiró P, Villa M, Botrugno OA, Dessanti P, Minucci S, Vultaggio S, Zagarrí E, Varasi M, Mercurio C.

J Med Chem. 2017 Mar 9;60(5):1693-1715. doi: 10.1021/acs.jmedchem.6b01019. Epub 2017 Feb 27.

PMID:
28186757
5.

Thieno[3,2-b]pyrrole-5-carboxamides as New Reversible Inhibitors of Histone Lysine Demethylase KDM1A/LSD1. Part 1: High-Throughput Screening and Preliminary Exploration.

Sartori L, Mercurio C, Amigoni F, Cappa A, Fagá G, Fattori R, Legnaghi E, Ciossani G, Mattevi A, Meroni G, Moretti L, Cecatiello V, Pasqualato S, Romussi A, Thaler F, Trifiró P, Villa M, Vultaggio S, Botrugno OA, Dessanti P, Minucci S, Zagarrí E, Carettoni D, Iuzzolino L, Varasi M, Vianello P.

J Med Chem. 2017 Mar 9;60(5):1673-1692. doi: 10.1021/acs.jmedchem.6b01018. Epub 2017 Feb 27.

PMID:
28186755
6.

T1 mapping with cardiovascular magnetic resonance: an emerging clinical biomarker.

Canepa M, Vianello PF, Abraham TP.

Heart. 2017 Feb 15;103(4):326. doi: 10.1136/heartjnl-2016-310678. No abstract available.

PMID:
28130438
7.

Distinguishing ventricular septal bulge versus hypertrophic cardiomyopathy in the elderly.

Canepa M, Pozios I, Vianello PF, Ameri P, Brunelli C, Ferrucci L, Abraham TP.

Heart. 2016 Jul 15;102(14):1087-94. doi: 10.1136/heartjnl-2015-308764. Epub 2016 Apr 27. Review.

8.

Discovery of a Novel Inhibitor of Histone Lysine-Specific Demethylase 1A (KDM1A/LSD1) as Orally Active Antitumor Agent.

Vianello P, Botrugno OA, Cappa A, Dal Zuffo R, Dessanti P, Mai A, Marrocco B, Mattevi A, Meroni G, Minucci S, Stazi G, Thaler F, Trifiró P, Valente S, Villa M, Varasi M, Mercurio C.

J Med Chem. 2016 Feb 25;59(4):1501-17. doi: 10.1021/acs.jmedchem.5b01209. Epub 2016 Jan 7.

PMID:
26702542
9.

Diagnostic value of ischemia severity at myocardial perfusion imaging in elderly persons with suspected coronary disease.

Canepa M, Bezante G, Vianello P, Ameri P, Milaneschi Y, Aste M, Cavalla F, Bauckneht M, Marini C, Balbi M, Brunelli C, Sambuceti G.

J Cardiovasc Med (Hagerstown). 2016 Oct;17(10):719-28. doi: 10.2459/JCM.0000000000000339.

PMID:
26599683
10.

Pure enantiomers of benzoylamino-tranylcypromine: LSD1 inhibition, gene modulation in human leukemia cells and effects on clonogenic potential of murine promyelocytic blasts.

Valente S, Rodriguez V, Mercurio C, Vianello P, Saponara B, Cirilli R, Ciossani G, Labella D, Marrocco B, Monaldi D, Ruoppolo G, Tilset M, Botrugno OA, Dessanti P, Minucci S, Mattevi A, Varasi M, Mai A.

Eur J Med Chem. 2015 Apr 13;94:163-74. doi: 10.1016/j.ejmech.2015.02.060. Epub 2015 Mar 3.

PMID:
25768700
11.

Pure Diastereomers of a Tranylcypromine-Based LSD1 Inhibitor: Enzyme Selectivity and In-Cell Studies.

Valente S, Rodriguez V, Mercurio C, Vianello P, Saponara B, Cirilli R, Ciossani G, Labella D, Marrocco B, Ruoppolo G, Botrugno OA, Dessanti P, Minucci S, Mattevi A, Varasi M, Mai A.

ACS Med Chem Lett. 2014 Dec 8;6(2):173-7. doi: 10.1021/ml500424z. eCollection 2015 Feb 12.

12.

Further insights into the SAR of α-substituted cyclopropylamine derivatives as inhibitors of histone demethylase KDM1A.

Pieroni M, Annunziato G, Azzali E, Dessanti P, Mercurio C, Meroni G, Trifiró P, Vianello P, Villa M, Beato C, Varasi M, Costantino G.

Eur J Med Chem. 2015 Mar 6;92:377-86. doi: 10.1016/j.ejmech.2014.12.032. Epub 2015 Jan 7.

PMID:
25585008
13.

Synthesis, biological activity and mechanistic insights of 1-substituted cyclopropylamine derivatives: a novel class of irreversible inhibitors of histone demethylase KDM1A.

Vianello P, Botrugno OA, Cappa A, Ciossani G, Dessanti P, Mai A, Mattevi A, Meroni G, Minucci S, Thaler F, Tortorici M, Trifiró P, Valente S, Villa M, Varasi M, Mercurio C.

Eur J Med Chem. 2014 Oct 30;86:352-63. doi: 10.1016/j.ejmech.2014.08.068. Epub 2014 Aug 27.

PMID:
25173853
14.

Pyrrole-3-carboxamides as potent and selective JAK2 inhibitors.

Brasca MG, Nesi M, Avanzi N, Ballinari D, Bandiera T, Bertrand J, Bindi S, Canevari G, Carenzi D, Casero D, Ceriani L, Ciomei M, Cirla A, Colombo M, Cribioli S, Cristiani C, Della Vedova F, Fachin G, Fasolini M, Felder ER, Galvani A, Isacchi A, Mirizzi D, Motto I, Panzeri A, Pesenti E, Vianello P, Gnocchi P, Donati D.

Bioorg Med Chem. 2014 Sep 1;22(17):4998-5012. doi: 10.1016/j.bmc.2014.06.025. Epub 2014 Jun 21.

PMID:
25009002
15.

Identification of a phenylacylsulfonamide series of dual Bcl-2/Bcl-xL antagonists.

Perez HL, Banfi P, Bertrand J, Cai ZW, Grebinski JW, Kim K, Lippy J, Modugno M, Naglich J, Schmidt RJ, Tebben A, Vianello P, Wei DD, Zhang L, Galvani A, Lombardo LJ, Borzilleri RM.

Bioorg Med Chem Lett. 2012 Jun 15;22(12):3946-50. doi: 10.1016/j.bmcl.2012.04.103. Epub 2012 May 2.

PMID:
22608961
16.

Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.

Menichincheri M, Albanese C, Alli C, Ballinari D, Bargiotti A, Caldarelli M, Ciavolella A, Cirla A, Colombo M, Colotta F, Croci V, D'Alessio R, D'Anello M, Ermoli A, Fiorentini F, Forte B, Galvani A, Giordano P, Isacchi A, Martina K, Molinari A, Moll JK, Montagnoli A, Orsini P, Orzi F, Pesenti E, Pillan A, Roletto F, Scolaro A, Tatò M, Tibolla M, Valsasina B, Varasi M, Vianello P, Volpi D, Santocanale C, Vanotti E.

J Med Chem. 2010 Oct 28;53(20):7296-315. doi: 10.1021/jm100504d.

PMID:
20873740
17.

Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.

Bindi S, Fancelli D, Alli C, Berta D, Bertrand JA, Cameron AD, Cappella P, Carpinelli P, Cervi G, Croci V, D'Anello M, Forte B, Giorgini ML, Marsiglio A, Moll J, Pesenti E, Pittalà V, Pulici M, Riccardi-Sirtori F, Roletto F, Soncini C, Storici P, Varasi M, Volpi D, Zugnoni P, Vianello P.

Bioorg Med Chem. 2010 Oct 1;18(19):7113-20. doi: 10.1016/j.bmc.2010.07.048. Epub 2010 Jul 25.

PMID:
20817473
18.

Identification of N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor.

Brasca MG, Amboldi N, Ballinari D, Cameron A, Casale E, Cervi G, Colombo M, Colotta F, Croci V, D'Alessio R, Fiorentini F, Isacchi A, Mercurio C, Moretti W, Panzeri A, Pastori W, Pevarello P, Quartieri F, Roletto F, Traquandi G, Vianello P, Vulpetti A, Ciomei M.

J Med Chem. 2009 Aug 27;52(16):5152-63. doi: 10.1021/jm9006559.

PMID:
19603809
19.

Optimization of pyrazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1).

Huynh T, Chen Z, Pang S, Geng J, Bandiera T, Bindi S, Vianello P, Roletto F, Thieffine S, Galvani A, Vaccaro W, Poss MA, Trainor GL, Lorenzi MV, Gottardis M, Jayaraman L, Purandare AV.

Bioorg Med Chem Lett. 2009 Jun 1;19(11):2924-7. doi: 10.1016/j.bmcl.2009.04.075. Epub 2009 Apr 22.

PMID:
19419866
20.

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.

21.

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, Zugnoni P, Vianello P.

J Med Chem. 2006 Nov 30;49(24):7247-51.

PMID:
17125279
22.

PHA-680632, a novel Aurora kinase inhibitor with potent antitumoral 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.

Clin Cancer Res. 2006 Jul 1;12(13):4080-9.

23.

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, Brasca MG.

Bioorg Med Chem Lett. 2006 Feb 15;16(4):1084-90. Epub 2005 Nov 14.

PMID:
16290148
24.

Classical and new proving methodology: provings of Plumbum metallicum and Piper methysticum and comparison with a classical proving of Plumbum metallicum.

Signorini A, Lubrano A, Manuele G, Fagone G, Vittorini C, Boso F, Vianello P, Rebuffi A, Frongia T, Rocco V, Pichler C.

Homeopathy. 2005 Jul;94(3):164-74.

PMID:
16060202
25.

Potent and selective Aurora 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, Vianello P.

J Med Chem. 2005 Apr 21;48(8):3080-4.

PMID:
15828847
26.

Solid-phase synthesis of a small library of 3-phenylthio-3-nicotinyl propionic acid derivatives acting as antagonists of the integrin alphaVbeta3.

Vianello P, Cozzi P, Galvani A, Meroni M, Varasi M, Volpi D, Bandiera T.

Bioorg Med Chem Lett. 2004 Feb 9;14(3):657-61.

PMID:
14741263
27.

Synthesis, modelling, and mu-opioid receptor affinity of N-3(9)-arylpropenyl-N-9(3)-propionyl-3,9-diazabicycl.

Pinna GA, Murineddu G, Curzu MM, Villa S, Vianello P, Borea PA, Gessi S, Toma L, Colombo D, Cignarella G.

Farmaco. 2000 Aug;55(8):553-62.

PMID:
11132733
28.

Synthesis, molecular modeling, and opioid receptor affinity of 9, 10-diazatricyclo[4.2.1.1(2,5)]decanes and 2,7-diazatricyclo[4.4.0. 0(3,8)]decanes structurally related to 3,8-diazabicyclo[3.2. 1]octanes.

Vianello P, Albinati A, Pinna GA, Lavecchia A, Marinelli L, Borea PA, Gessi S, Fadda P, Tronci S, Cignarella G.

J Med Chem. 2000 Jun 1;43(11):2115-23.

PMID:
10841790
29.

Isoxazolo-[3,4-d]-pyridazin-7-(6H)-one as a potential substrate for new aldose reductase inhibitors.

Costantino L, Rastelli G, Gamberini MC, Giovannoni MP, Dal Piaz V, Vianello P, Barlocco D.

J Med Chem. 1999 Jun 3;42(11):1894-900.

PMID:
10354397
30.
31.

Benzocondensed derivatives as rigid analogues of the mu-opioid agonist 3(8)-cinnamyl-8(3)-propionyl-3,8-diazabicyclo[3.2.1]octanes: synthesis, modeling, and affinity.

Cignarella G, Barlocco D, Vianello P, Villa S, Pinna GA, Fadda P, Fratta W, Toma L, Gessi S.

Farmaco. 1998 Oct-Nov;53(10-11):667-74.

PMID:
10205853
32.

Synthesis and mu-opioid receptor affinity of a new series of nitro substituted 3,8-diazabicyclo[3.2.1]octane derivatives.

Barlocco D, Cignarella G, Vianello P, Villa S, Pinna GA, Fadda P, Fratta W.

Farmaco. 1998 Aug-Sep;53(8-9):557-62.

PMID:
10081818
33.

Diabetes complications and their potential prevention: aldose reductase inhibition and other approaches.

Costantino L, Rastelli G, Vianello P, Cignarella G, Barlocco D.

Med Res Rev. 1999 Jan;19(1):3-23. Review.

PMID:
9918192
34.

Generation of specific deoxynojirimycin-type inhibitors of the non-lysosomal glucosylceramidase.

Overkleeft HS, Renkema GH, Neele J, Vianello P, Hung IO, Strijland A, van der Burg AM, Koomen GJ, Pandit UK, Aerts JM.

J Biol Chem. 1998 Oct 9;273(41):26522-7.

35.

Mono- and disubstituted-3,8-diazabicyclo[3.2.1]octane derivatives as analgesics structurally related to epibatidine: synthesis, activity, and modeling.

Barlocco D, Cignarella G, Tondi D, Vianello P, Villa S, Bartolini A, Ghelardini C, Galeotti N, Anderson DJ, Kuntzweiler TA, Colombo D, Toma L.

J Med Chem. 1998 Feb 26;41(5):674-81.

PMID:
9513595
36.

Indenopyridazinone derivatives as potential antisecretory and antiulcer agents.

Barlocco D, Cignarella G, Vianello P, Dal Piaz V, Giovannoni MP, Malandrino S, Barocelli E, Chiavarini M, Impicciatore M.

Drug Des Discov. 1997 Aug;15(2):95-103.

PMID:
9342552
37.

Study of the antisecretory and antiulcer mechanisms of a new indenopirydazinone derivative in rats.

Barocelli E, Chiavarini M, Ballabeni V, Barlocco D, Vianello P, Dal Piaz V, Impicciatore M.

Pharmacol Res. 1997 May;35(5):487-92.

PMID:
9299216
38.

Synthesis, activity, and molecular modeling of a new series of tricyclic pyridazinones as selective aldose reductase inhibitors.

Costantino L, Rastelli G, Vescovini K, Cignarella G, Vianello P, Del Corso A, Cappiello M, Mura U, Barlocco D.

J Med Chem. 1996 Oct 25;39(22):4396-405.

PMID:
8893834

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