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Items: 1 to 50 of 86

1.

2-Phenylquinazolinones as dual-activity tankyrase-kinase inhibitors.

Nkizinkiko Y, Desantis J, Koivunen J, Haikarainen T, Murthy S, Sancineto L, Massari S, Ianni F, Obaji E, Loza MI, Pihlajaniemi T, Brea J, Tabarrini O, Lehtiö L.

Sci Rep. 2018 Jan 26;8(1):1680. doi: 10.1038/s41598-018-19872-3.

2.

NCp7: targeting a multitask protein for next-generation anti-HIV drug development part 2. Noncovalent inhibitors and nucleic acid binders.

Iraci N, Tabarrini O, Santi C, Sancineto L.

Drug Discov Today. 2018 Jan 8. pii: S1359-6446(17)30369-0. doi: 10.1016/j.drudis.2018.01.022. [Epub ahead of print] Review.

PMID:
29326078
3.

Editorial: Acting on Tat-Mediated Transcription to Achieve a Long Term Control of HIV-1 Latency.

Tabarrini O, Massari S.

Curr Pharm Des. 2017 Nov 2. doi: 10.2174/138161282328171102111432. [Epub ahead of print] No abstract available.

PMID:
29210645
4.

Functionalized 2,1-benzothiazine 2,2-dioxides as new inhibitors of Dengue NS5 RNA-dependent RNA polymerase.

Cannalire R, Tarantino D, Astolfi A, Barreca ML, Sabatini S, Massari S, Tabarrini O, Milani M, Querat G, Mastrangelo E, Manfroni G, Cecchetti V.

Eur J Med Chem. 2018 Jan 1;143:1667-1676. doi: 10.1016/j.ejmech.2017.10.064. Epub 2017 Nov 11.

PMID:
29137867
5.

NCp7: targeting a multitasking protein for next-generation anti-HIV drug development part 1: covalent inhibitors.

Sancineto L, Iraci N, Tabarrini O, Santi C.

Drug Discov Today. 2018 Feb;23(2):260-271. doi: 10.1016/j.drudis.2017.10.017. Epub 2017 Oct 28. Review.

PMID:
29107765
6.

Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.

Cannalire R, Machado D, Felicetti T, Santos Costa S, Massari S, Manfroni G, Barreca ML, Tabarrini O, Couto I, Viveiros M, Sabatini S, Cecchetti V.

Eur J Med Chem. 2017 Nov 10;140:321-330. doi: 10.1016/j.ejmech.2017.09.014. Epub 2017 Sep 12.

PMID:
28964936
7.

Efficient and regioselective one-step synthesis of 7-aryl-5-methyl- and 5-aryl-7-methyl-2-amino-[1,2,4]triazolo[1,5-a]pyrimidine derivatives.

Massari S, Desantis J, Nannetti G, Sabatini S, Tortorella S, Goracci L, Cecchetti V, Loregian A, Tabarrini O.

Org Biomol Chem. 2017 Sep 26;15(37):7944-7955. doi: 10.1039/c7ob02085f.

PMID:
28902220
8.

Exploring the cycloheptathiophene-3-carboxamide scaffold to disrupt the interactions of the influenza polymerase subunits and obtain potent anti-influenza activity.

Desantis J, Nannetti G, Massari S, Barreca ML, Manfroni G, Cecchetti V, Palù G, Goracci L, Loregian A, Tabarrini O.

Eur J Med Chem. 2017 Sep 29;138:128-139. doi: 10.1016/j.ejmech.2017.06.015. Epub 2017 Jun 8.

PMID:
28666191
9.

Halogen Bonding in Nucleic Acid Complexes.

Kolář MH, Tabarrini O.

J Med Chem. 2017 Nov 9;60(21):8681-8690. doi: 10.1021/acs.jmedchem.7b00329. Epub 2017 Jun 23.

PMID:
28605588
10.

Searching for Novel Inhibitors of the S. aureus NorA Efflux Pump: Synthesis and Biological Evaluation of the 3-Phenyl-1,4-benzothiazine Analogues.

Felicetti T, Cannalire R, Burali MS, Massari S, Manfroni G, Barreca ML, Tabarrini O, Schindler BD, Sabatini S, Kaatz GW, Cecchetti V.

ChemMedChem. 2017 Aug 22;12(16):1293-1302. doi: 10.1002/cmdc.201700286. Epub 2017 Jul 17.

PMID:
28598572
11.

Mode of action of the 2-phenylquinoline efflux inhibitor PQQ4R against Escherichia coli.

Machado D, Fernandes L, Costa SS, Cannalire R, Manfroni G, Tabarrini O, Couto I, Sabatini S, Viveiros M.

PeerJ. 2017 Apr 26;5:e3168. doi: 10.7717/peerj.3168. eCollection 2017.

12.

Pharmacophore-Based Repositioning of Approved Drugs as Novel Staphylococcus aureus NorA Efflux Pump Inhibitors.

Astolfi A, Felicetti T, Iraci N, Manfroni G, Massari S, Pietrella D, Tabarrini O, Kaatz GW, Barreca ML, Sabatini S, Cecchetti V.

J Med Chem. 2017 Feb 23;60(4):1598-1604. doi: 10.1021/acs.jmedchem.6b01439. Epub 2017 Feb 8.

PMID:
28117588
13.

Boosting Effect of 2-Phenylquinoline Efflux Inhibitors in Combination with Macrolides against Mycobacterium smegmatis and Mycobacterium avium.

Machado D, Cannalire R, Santos Costa S, Manfroni G, Tabarrini O, Cecchetti V, Couto I, Viveiros M, Sabatini S.

ACS Infect Dis. 2015 Dec 11;1(12):593-603. doi: 10.1021/acsinfecdis.5b00052. Epub 2015 Jul 23.

PMID:
27623057
14.

Polymerase Acidic Protein-Basic Protein 1 (PA-PB1) Protein-Protein Interaction as a Target for Next-Generation Anti-influenza Therapeutics.

Massari S, Goracci L, Desantis J, Tabarrini O.

J Med Chem. 2016 Sep 8;59(17):7699-718. doi: 10.1021/acs.jmedchem.5b01474. Epub 2016 Apr 19. Review.

PMID:
27046062
15.

Studies on Cycloheptathiophene-3-carboxamide Derivatives as Allosteric HIV-1 Ribonuclease H Inhibitors.

Corona A, Desantis J, Massari S, Distinto S, Masaoka T, Sabatini S, Esposito F, Manfroni G, Maccioni E, Cecchetti V, Pannecouque C, Le Grice SF, Tramontano E, Tabarrini O.

ChemMedChem. 2016 Aug 19;11(16):1709-20. doi: 10.1002/cmdc.201600015. Epub 2016 Mar 16.

PMID:
26990134
16.

Recent advances in the identification of Tat-mediated transactivation inhibitors: progressing toward a functional cure of HIV.

Tabarrini O, Desantis J, Massari S.

Future Med Chem. 2016;8(4):421-42. doi: 10.4155/fmc.16.3. Epub 2016 Mar 2. Review.

PMID:
26933891
17.

Drug Repurposing Approach Identifies Inhibitors of the Prototypic Viral Transcription Factor IE2 that Block Human Cytomegalovirus Replication.

Mercorelli B, Luganini A, Nannetti G, Tabarrini O, Palù G, Gribaudo G, Loregian A.

Cell Chem Biol. 2016 Mar 17;23(3):340-51. doi: 10.1016/j.chembiol.2015.12.012. Epub 2016 Feb 11.

18.

A new vinyl selenone-based domino approach to spirocyclopropyl oxindoles endowed with anti-HIV RT activity.

Palomba M, Rossi L, Sancineto L, Tramontano E, Corona A, Bagnoli L, Santi C, Pannecouque C, Tabarrini O, Marini F.

Org Biomol Chem. 2016 Feb 14;14(6):2015-24. doi: 10.1039/c5ob02451j.

PMID:
26754878
19.

Design and Synthesis of DiselenoBisBenzamides (DISeBAs) as Nucleocapsid Protein 7 (NCp7) Inhibitors with anti-HIV Activity.

Sancineto L, Mariotti A, Bagnoli L, Marini F, Desantis J, Iraci N, Santi C, Pannecouque C, Tabarrini O.

J Med Chem. 2015 Dec 24;58(24):9601-14. doi: 10.1021/acs.jmedchem.5b01183. Epub 2015 Dec 10.

PMID:
26613134
20.

Tumour cell population growth inhibition and cell death induction of functionalized 6-aminoquinolone derivatives.

Franci G, Manfroni G, Cannalire R, Felicetti T, Tabarrini O, Salvato A, Barreca ML, Altucci L, Cecchetti V.

Cell Prolif. 2015 Dec;48(6):705-17. doi: 10.1111/cpr.12224.

PMID:
26597381
21.

Molecular view of ligands specificity for CAG repeats in anti-Huntington therapy.

Bochicchio A, Rossetti G, Tabarrini O, Krauβ S, Carloni P.

J Chem Theory Comput. 2015 Oct 13;11(10):4911-22. doi: 10.1021/acs.jctc.5b00208. Epub 2015 Sep 10.

PMID:
26574279
22.

A Broad Anti-influenza Hybrid Small Molecule That Potently Disrupts the Interaction of Polymerase Acidic Protein-Basic Protein 1 (PA-PB1) Subunits.

Massari S, Nannetti G, Desantis J, Muratore G, Sabatini S, Manfroni G, Mercorelli B, Cecchetti V, Palù G, Cruciani G, Loregian A, Goracci L, Tabarrini O.

J Med Chem. 2015 May 14;58(9):3830-42. doi: 10.1021/acs.jmedchem.5b00012. Epub 2015 Apr 20.

PMID:
25856229
23.

The Pyrazolobenzothiazine Core as a New Chemotype of p38 Alpha Mitogen-Activated Protein Kinase Inhibitors.

Sabatini S, Manfroni G, Barreca ML, Bauer SM, Gargaro M, Cannalire R, Astolfi A, Brea J, Vacca C, Pirro M, Massari S, Tabarrini O, Loza MI, Fallarino F, Laufer SA, Cecchetti V.

Chem Biol Drug Des. 2015 Oct;86(4):531-45. doi: 10.1111/cbdd.12516. Epub 2015 Feb 19.

PMID:
25589097
24.

The 6-Aminoquinolone WC5 inhibits different functions of the immediate-early 2 (IE2) protein of human cytomegalovirus that are essential for viral replication.

Mercorelli B, Luganini A, Muratore G, Massari S, Terlizzi ME, Tabarrini O, Gribaudo G, Palù G, Loregian A.

Antimicrob Agents Chemother. 2014 Nov;58(11):6615-26. doi: 10.1128/AAC.03309-14. Epub 2014 Aug 25.

25.

Exploiting the anti-HIV 6-desfluoroquinolones to design multiple ligands.

Sancineto L, Iraci N, Barreca ML, Massari S, Manfroni G, Corazza G, Cecchetti V, Marcello A, Daelemans D, Pannecouque C, Tabarrini O.

Bioorg Med Chem. 2014 Sep 1;22(17):4658-66. doi: 10.1016/j.bmc.2014.07.018. Epub 2014 Jul 22.

PMID:
25127466
26.

Ethyl 1,8-naphthyridone-3-carboxylates downregulate human papillomavirus-16 E6 and E7 oncogene expression.

Donalisio M, Massari S, Argenziano M, Manfroni G, Cagno V, Civra A, Sabatini S, Cecchetti V, Loregian A, Cavalli R, Lembo D, Tabarrini O.

J Med Chem. 2014 Jul 10;57(13):5649-63. doi: 10.1021/jm500340h. Epub 2014 Jun 25.

27.

New pyrazolobenzothiazine derivatives as hepatitis C virus NS5B polymerase palm site I inhibitors.

Manfroni G, Manvar D, Barreca ML, Kaushik-Basu N, Leyssen P, Paeshuyse J, Cannalire R, Iraci N, Basu A, Chudaev M, Zamperini C, Dreassi E, Sabatini S, Tabarrini O, Neyts J, Cecchetti V.

J Med Chem. 2014 Apr 24;57(8):3247-62. doi: 10.1021/jm401688h. Epub 2014 Apr 2.

28.

Structural investigation of cycloheptathiophene-3-carboxamide derivatives targeting influenza virus polymerase assembly.

Massari S, Nannetti G, Goracci L, Sancineto L, Muratore G, Sabatini S, Manfroni G, Mercorelli B, Cecchetti V, Facchini M, Palù G, Cruciani G, Loregian A, Tabarrini O.

J Med Chem. 2013 Dec 27;56(24):10118-31. doi: 10.1021/jm401560v. Epub 2013 Dec 13.

PMID:
24313730
29.

Modulation of HIV-1-induced activation of plasmacytoid dendritic cells by 6-desfluoroquinolones.

Royle CM, Tsai MH, Tabarrini O, Massari S, Graham DR, Aquino VN, Boasso A.

AIDS Res Hum Retroviruses. 2014 Apr;30(4):345-54. doi: 10.1089/AID.2013.0154. Epub 2013 Dec 9.

30.

Computer-aided design, synthesis and validation of 2-phenylquinazolinone fragments as CDK9 inhibitors with anti-HIV-1 Tat-mediated transcription activity.

Sancineto L, Iraci N, Massari S, Attanasio V, Corazza G, Barreca ML, Sabatini S, Manfroni G, Avanzi NR, Cecchetti V, Pannecouque C, Marcello A, Tabarrini O.

ChemMedChem. 2013 Dec;8(12):1941-53. doi: 10.1002/cmdc.201300287. Epub 2013 Oct 21.

PMID:
24150998
31.

The versatile nature of the 6-aminoquinolone scaffold: identification of submicromolar hepatitis C virus NS5B inhibitors.

Manfroni G, Cannalire R, Barreca ML, Kaushik-Basu N, Leyssen P, Winquist J, Iraci N, Manvar D, Paeshuyse J, Guhamazumder R, Basu A, Sabatini S, Tabarrini O, Danielson UH, Neyts J, Cecchetti V.

J Med Chem. 2014 Mar 13;57(5):1952-63. doi: 10.1021/jm401362f. Epub 2013 Nov 6.

32.

Accounting for target flexibility and water molecules by docking to ensembles of target structures: the HCV NS5B palm site I inhibitors case study.

Barreca ML, Iraci N, Manfroni G, Gaetani R, Guercini C, Sabatini S, Tabarrini O, Cecchetti V.

J Chem Inf Model. 2014 Feb 24;54(2):481-97. doi: 10.1021/ci400367m. Epub 2013 Sep 5.

PMID:
23952658
33.

Design, synthesis, and evaluation of WC5 analogues as inhibitors of human cytomegalovirus Immediate-Early 2 protein, a promising target for anti-HCMV treatment.

Massari S, Mercorelli B, Sancineto L, Sabatini S, Cecchetti V, Gribaudo G, Palù G, Pannecouque C, Loregian A, Tabarrini O.

ChemMedChem. 2013 Aug;8(8):1403-14. doi: 10.1002/cmdc.201300106. Epub 2013 Jun 11.

PMID:
23757191
34.

Re-evolution of the 2-phenylquinolines: ligand-based design, synthesis, and biological evaluation of a potent new class of Staphylococcus aureus NorA efflux pump inhibitors to combat antimicrobial resistance.

Sabatini S, Gosetto F, Iraci N, Barreca ML, Massari S, Sancineto L, Manfroni G, Tabarrini O, Dimovska M, Kaatz GW, Cecchetti V.

J Med Chem. 2013 Jun 27;56(12):4975-89. doi: 10.1021/jm400262a. Epub 2013 Jun 13.

PMID:
23710549
35.

1,4-Benzothiazine ATP-sensitive potassium channel openers: modifications at the C-2 and C-6 positions.

Martelli A, Manfroni G, Sabbatini P, Barreca ML, Testai L, Novelli M, Sabatini S, Massari S, Tabarrini O, Masiello P, Calderone V, Cecchetti V.

J Med Chem. 2013 Jun 13;56(11):4718-28. doi: 10.1021/jm400435a. Epub 2013 May 28.

PMID:
23662847
36.

From small to powerful: the fragments universe and its "chem-appeal".

Sancineto L, Massari S, Iraci N, Tabarrini O.

Curr Med Chem. 2013;20(11):1355-81. Review.

PMID:
23410157
37.

Structure-based discovery of pyrazolobenzothiazine derivatives as inhibitors of hepatitis C virus replication.

Barreca ML, Manfroni G, Leyssen P, Winquist J, Kaushik-Basu N, Paeshuyse J, Krishnan R, Iraci N, Sabatini S, Tabarrini O, Basu A, Danielson UH, Neyts J, Cecchetti V.

J Med Chem. 2013 Mar 28;56(6):2270-82. doi: 10.1021/jm301643a. Epub 2013 Mar 7.

38.

Blocking HIV-1 replication by targeting the Tat-hijacked transcriptional machinery.

Massari S, Sabatini S, Tabarrini O.

Curr Pharm Des. 2013;19(10):1860-79. Review.

PMID:
23092279
39.

6-hydrogen-8-methylquinolones active against replicating and non-replicating Mycobacterium tuberculosis.

Tabarrini O, Sabatini S, Massari S, Pieroni M, Franzblau SG, Cecchetti V.

Chem Biol Drug Des. 2012 Nov;80(5):781-6. doi: 10.1111/cbdd.12022. Epub 2012 Sep 10.

PMID:
22889240
40.

Pyrazolo[4,3-c][1,2]benzothiazines 5,5-dioxide: a promising new class of Staphylococcus aureus NorA efflux pump inhibitors.

Sabatini S, Gosetto F, Serritella S, Manfroni G, Tabarrini O, Iraci N, Brincat JP, Carosati E, Villarini M, Kaatz GW, Cecchetti V.

J Med Chem. 2012 Apr 12;55(7):3568-72. doi: 10.1021/jm201446h. Epub 2012 Apr 3.

PMID:
22432682
41.

Synthesis and chromatographic enantioresolution of anti-HIV quinolone derivatives.

Natalini B, Sardella R, Massari S, Ianni F, Tabarrini O, Cecchetti V.

Talanta. 2011 Sep 15;85(3):1392-7. doi: 10.1016/j.talanta.2011.06.047. Epub 2011 Jun 22.

PMID:
21807200
42.

Evolution from a natural flavones nucleus to obtain 2-(4-Propoxyphenyl)quinoline derivatives as potent inhibitors of the S. aureus NorA efflux pump.

Sabatini S, Gosetto F, Manfroni G, Tabarrini O, Kaatz GW, Patel D, Cecchetti V.

J Med Chem. 2011 Aug 25;54(16):5722-36. doi: 10.1021/jm200370y. Epub 2011 Aug 3.

PMID:
21751791
43.

Structural investigation of the naphthyridone scaffold: identification of a 1,6-naphthyridone derivative with potent and selective anti-HIV activity.

Tabarrini O, Massari S, Sancineto L, Daelemans D, Sabatini S, Manfroni G, Cecchetti V, Pannecouque C.

ChemMedChem. 2011 Jul 4;6(7):1249-57. doi: 10.1002/cmdc.201100073. Epub 2011 May 12.

PMID:
21567967
44.

6-desfluoroquinolones as HIV-1 Tat-mediated transcription inhibitors.

Tabarrini O, Massari S, Cecchetti V.

Future Med Chem. 2010 Jul;2(7):1161-80. doi: 10.4155/fmc.10.208. Review.

PMID:
21426162
45.

Studies of anti-HIV transcription inhibitor quinolones: identification of potent N1-vinyl derivatives.

Tabarrini O, Massari S, Daelemans D, Meschini F, Manfroni G, Bottega L, Gatto B, Palumbo M, Pannecouque C, Cecchetti V.

ChemMedChem. 2010 Nov 8;5(11):1880-92. doi: 10.1002/cmdc.201000267.

PMID:
20928882
46.

The 6-aminoquinolone WC5 inhibits human cytomegalovirus replication at an early stage by interfering with the transactivating activity of viral immediate-early 2 protein.

Loregian A, Mercorelli B, Muratore G, Sinigalia E, Pagni S, Massari S, Gribaudo G, Gatto B, Palumbo M, Tabarrini O, Cecchetti V, Palù G.

Antimicrob Agents Chemother. 2010 May;54(5):1930-40. doi: 10.1128/AAC.01730-09. Epub 2010 Mar 1.

47.

A 1,8-naphthyridone derivative targets the HIV-1 Tat-mediated transcription and potently inhibits the HIV-1 replication.

Massari S, Daelemans D, Barreca ML, Knezevich A, Sabatini S, Cecchetti V, Marcello A, Pannecouque C, Tabarrini O.

J Med Chem. 2010 Jan 28;53(2):641-8. doi: 10.1021/jm901211d.

PMID:
19958026
48.

Inhibition of subgenomic hepatitis C virus RNA replication by acridone derivatives: identification of an NS3 helicase inhibitor.

Manfroni G, Paeshuyse J, Massari S, Zanoli S, Gatto B, Maga G, Tabarrini O, Cecchetti V, Fravolini A, Neyts J.

J Med Chem. 2009 May 28;52(10):3354-65. doi: 10.1021/jm801608u.

PMID:
19388645
49.

2-Phenylquinolones as inhibitors of the HIV-1 Tat-TAR interaction.

Gatto B, Tabarrini O, Massari S, Giaretta G, Sabatini S, Del Vecchio C, Parolin C, Fravolini A, Palumbo M, Cecchetti V.

ChemMedChem. 2009 Jun;4(6):935-8. doi: 10.1002/cmdc.200800437.

PMID:
19283692
50.

Synthesis and biological evaluation of 2-phenylquinolones targeted at Tat/TAR recognition.

Manfroni G, Gatto B, Tabarrini O, Sabatini S, Cecchetti V, Giaretta G, Parolin C, Del Vecchio C, Calistri A, Palumbo M, Fravolini A.

Bioorg Med Chem Lett. 2009 Feb 1;19(3):714-7. doi: 10.1016/j.bmcl.2008.12.034. Epub 2008 Dec 11.

PMID:
19109014

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