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Synthesis, Molecular Modelling and Biological Studies of 3-hydroxy-pyrane-4-one and 3-hydroxy-pyridine-4-one Derivatives as HIV-1 Integrase Inhibitors.

Sirous H, Fassihi A, Brogi S, Campiani G, Christ F, Debyser Z, Gemma S, Butini S, Chemi G, Grillo A, Zabihollahi R, Aghasadeghi MR, Saghaie L, Memarian HR.

Med Chem. 2018 Dec 18. doi: 10.2174/1573406415666181219113225. [Epub ahead of print]


Author Correction: The FAAH inhibitor URB597 suppresses hippocampal maximal dentate afterdischarges and restores seizure-induced impairment of short and long-term synaptic plasticity.

Colangeli R, Pierucci M, Benigno A, Campiani G, Butini S, Di Giovanni G.

Sci Rep. 2018 Dec 14;8(1):17977. doi: 10.1038/s41598-018-37392-y.


Structure-activity relationships, biological evaluation and structural studies of novel pyrrolonaphthoxazepines as antitumor agents.

Brindisi M, Ulivieri C, Alfano G, Gemma S, de Asís Balaguer F, Khan T, Grillo A, Chemi G, Menchon G, Prota AE, Olieric N, Lucena-Agell D, Barasoain I, Diaz JF, Nebbioso A, Conte M, Lopresti L, Magnano S, Amet R, Kinsella P, Zisterer DM, Ibrahim O, O'Sullivan J, Morbidelli L, Spaccapelo R, Baldari C, Butini S, Novellino E, Campiani G, Altucci L, Steinmetz MO, Brogi S.

Eur J Med Chem. 2019 Jan 15;162:290-320. doi: 10.1016/j.ejmech.2018.11.004. Epub 2018 Nov 3.


Cinnamic acids derived compounds with antileishmanial activity target Leishmania amazonensis arginase.

da Silva ER, Brogi S, Grillo A, Campiani G, Gemma S, Vieira PC, Maquiaveli CDC.

Chem Biol Drug Des. 2019 Feb;93(2):139-146. doi: 10.1111/cbdd.13391. Epub 2018 Oct 10.


Development of a Multiplexed Activity-Based Protein Profiling Assay to Evaluate Activity of Endocannabinoid Hydrolase Inhibitors.

Janssen APA, van der Vliet D, Bakker AT, Jiang M, Grimm SH, Campiani G, Butini S, van der Stelt M.

ACS Chem Biol. 2018 Sep 21;13(9):2406-2413. doi: 10.1021/acschembio.8b00534. Epub 2018 Sep 12.


Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies.

Brindisi M, Senger J, Cavella C, Grillo A, Chemi G, Gemma S, Cucinella DM, Lamponi S, Sarno F, Iside C, Nebbioso A, Novellino E, Shaik TB, Romier C, Herp D, Jung M, Butini S, Campiani G, Altucci L, Brogi S.

Eur J Med Chem. 2018 Sep 5;157:127-138. doi: 10.1016/j.ejmech.2018.07.069. Epub 2018 Jul 31.


Development of Potent Inhibitors of Fatty Acid Amide Hydrolase Useful for the Treatment of Neuropathic Pain.

Brindisi M, Borrelli G, Brogi S, Grillo A, Maramai S, Paolino M, Benedusi M, Pecorelli A, Valacchi G, Di Cesare Mannelli L, Ghelardini C, Allarà M, Ligresti A, Minetti P, Campiani G, di Marzo V, Butini S, Gemma S.

ChemMedChem. 2018 Oct 8;13(19):2090-2103. doi: 10.1002/cmdc.201800397. Epub 2018 Aug 30.


iPSC-derived neurons profiling reveals GABAergic circuit disruption and acetylated α-tubulin defect which improves after iHDAC6 treatment in Rett syndrome.

Landucci E, Brindisi M, Bianciardi L, Catania LM, Daga S, Croci S, Frullanti E, Fallerini C, Butini S, Brogi S, Furini S, Melani R, Molinaro A, Lorenzetti FC, Imperatore V, Amabile S, Mariani J, Mari F, Ariani F, Pizzorusso T, Pinto AM, Vaccarino FM, Renieri A, Campiani G, Meloni I.

Exp Cell Res. 2018 Jul 15;368(2):225-235. doi: 10.1016/j.yexcr.2018.05.001. Epub 2018 May 4.


Antimalarial agents against both sexual and asexual parasites stages: structure-activity relationships and biological studies of the Malaria Box compound 1-[5-(4-bromo-2-chlorophenyl)furan-2-yl]-N-[(piperidin-4-yl)methyl]methanamine (MMV019918) and analogues.

Vallone A, D'Alessandro S, Brogi S, Brindisi M, Chemi G, Alfano G, Lamponi S, Lee SG, Jez JM, Koolen KJM, Dechering KJ, Saponara S, Fusi F, Gorelli B, Taramelli D, Parapini S, Caldelari R, Campiani G, Gemma S, Butini S.

Eur J Med Chem. 2018 Apr 25;150:698-718. doi: 10.1016/j.ejmech.2018.03.024. Epub 2018 Mar 10.


Author Correction: The FAAH inhibitor URB597 suppresses hippocampal maximal dentate afterdischarges and restores seizure-induced impairment of short and long-term synaptic plasticity.

Colangeli R, Pierucci M, Benigno A, Campiani G, Butini S, Di Giovanni G.

Sci Rep. 2018 Mar 12;8(1):4648. doi: 10.1038/s41598-018-23084-0.


( S)-2-Amino-3-(5-methyl-3-hydroxyisoxazol-4-yl)propanoic Acid (AMPA) and Kainate Receptor Ligands: Further Exploration of Bioisosteric Replacements and Structural and Biological Investigation.

Brogi S, Brindisi M, Butini S, Kshirsagar GU, Maramai S, Chemi G, Gemma S, Campiani G, Novellino E, Fiorenzani P, Pinassi J, Aloisi AM, Gynther M, Venskutonytė R, Han L, Frydenvang K, Kastrup JS, Pickering DS.

J Med Chem. 2018 Mar 8;61(5):2124-2130. doi: 10.1021/acs.jmedchem.8b00099. Epub 2018 Feb 26.


Development of Potent Inhibitors of the Mycobacterium tuberculosis Virulence Factor Zmp1 and Evaluation of Their Effect on Mycobacterial Survival inside Macrophages.

Paolino M, Brindisi M, Vallone A, Butini S, Campiani G, Nannicini C, Giuliani G, Anzini M, Lamponi S, Giorgi G, Sbardella D, Ferraris DM, Marini S, Coletta M, Palucci I, Minerva M, Delogu G, Pepponi I, Goletti D, Cappelli A, Gemma S, Brogi S.

ChemMedChem. 2018 Mar 6;13(5):422-430. doi: 10.1002/cmdc.201700759. Epub 2018 Feb 14.


Activation of the Wnt Pathway by Small Peptides: Rational Design, Synthesis and Biological Evaluation.

Brogi S, Maramai S, Brindisi M, Chemi G, Porcari V, Corallo C, Gennari L, Novellino E, Ramunno A, Butini S, Campiani G, Gemma S.

ChemMedChem. 2017 Dec 19;12(24):2074-2085. doi: 10.1002/cmdc.201700551. Epub 2017 Nov 29.


First dual AK/GSK-3β inhibitors endowed with antioxidant properties as multifunctional, potential neuroprotective agents.

Brogi S, Ramunno A, Savi L, Chemi G, Alfano G, Pecorelli A, Pambianchi E, Galatello P, Compagnoni G, Focher F, Biamonti G, Valacchi G, Butini S, Gemma S, Campiani G, Brindisi M.

Eur J Med Chem. 2017 Sep 29;138:438-457. doi: 10.1016/j.ejmech.2017.06.017. Epub 2017 Jun 9.


Computational Tool for Fast in silico Evaluation of hERG K+ Channel Affinity.

Chemi G, Gemma S, Campiani G, Brogi S, Butini S, Brindisi M.

Front Chem. 2017 Feb 23;5:7. doi: 10.3389/fchem.2017.00007. eCollection 2017.


Structural characterization of Giardia duodenalis thioredoxin reductase (gTrxR) and computational analysis of its interaction with NBDHEX.

Brogi S, Fiorillo A, Chemi G, Butini S, Lalle M, Ilari A, Gemma S, Campiani G.

Eur J Med Chem. 2017 Jul 28;135:479-490. doi: 10.1016/j.ejmech.2017.04.057. Epub 2017 Apr 24.


Pre-clinical evaluation of a novel class of anti-cancer agents, the Pyrrolo-1, 5-benzoxazepines.

Greene LM, Butini S, Campiani G, Williams DC, Zisterer DM.

J Cancer. 2016 Dec 4;7(15):2367-2377. eCollection 2016. Review.


Identification of novel fluorescent probes preventing PrPSc replication in prion diseases.

Zaccagnini L, Brogi S, Brindisi M, Gemma S, Chemi G, Legname G, Campiani G, Butini S.

Eur J Med Chem. 2017 Feb 15;127:859-873. doi: 10.1016/j.ejmech.2016.10.064. Epub 2016 Nov 1.


Dopamine D3 Receptor Antagonists as Potential Therapeutics for the Treatment of Neurological Diseases.

Maramai S, Gemma S, Brogi S, Campiani G, Butini S, Stark H, Brindisi M.

Front Neurosci. 2016 Oct 5;10:451. eCollection 2016. Review.


Phenylpyrrole-based HDAC inhibitors: synthesis, molecular modeling and biological studies.

Brindisi M, Cavella C, Brogi S, Nebbioso A, Senger J, Maramai S, Ciotta A, Iside C, Butini S, Lamponi S, Novellino E, Altucci L, Jung M, Campiani G, Gemma S.

Future Med Chem. 2016 Sep;8(13):1573-87. doi: 10.4155/fmc-2016-0068. Epub 2016 Aug 24.


Involvement of AMP-activated protein kinase in mediating pyrrolo-1,5-benzoxazepine-induced apoptosis in neuroblastoma cells.

Lennon JC, Butini S, Campiani G, O'Meara A, Williams DC, Zisterer DM.

Invest New Drugs. 2016 Oct;34(5):663-76. doi: 10.1007/s10637-016-0366-3. Epub 2016 Jun 22.


Polypharmacology of dopamine receptor ligands.

Butini S, Nikolic K, Kassel S, Brückmann H, Filipic S, Agbaba D, Gemma S, Brogi S, Brindisi M, Campiani G, Stark H.

Prog Neurobiol. 2016 Jul;142:68-103. doi: 10.1016/j.pneurobio.2016.03.011. Epub 2016 May 24. Review.


The pyrrolo-1,5-benzoxazepine, PBOX-15, enhances TRAIL‑induced apoptosis by upregulation of DR5 and downregulation of core cell survival proteins in acute lymphoblastic leukaemia cells.

Nathwani SM, Greene LM, Butini S, Campiani G, Williams DC, Samali A, Szegezdi E, Zisterer DM.

Int J Oncol. 2016 Jul;49(1):74-88. doi: 10.3892/ijo.2016.3518. Epub 2016 May 12.


Development of novel cyclic peptides as pro-apoptotic agents.

Brindisi M, Maramai S, Brogi S, Fanigliulo E, Butini S, Guarino E, Casagni A, Lamponi S, Bonechi C, Nathwani SM, Finetti F, Ragonese F, Arcidiacono P, Campiglia P, Valenti S, Novellino E, Spaccapelo R, Morbidelli L, Zisterer DM, Williams CD, Donati A, Baldari C, Campiani G, Ulivieri C, Gemma S.

Eur J Med Chem. 2016 Jul 19;117:301-20. doi: 10.1016/j.ejmech.2016.04.001. Epub 2016 Apr 5.


Targeting clinically-relevant metallo-β-lactamases: from high-throughput docking to broad-spectrum inhibitors.

Brindisi M, Brogi S, Giovani S, Gemma S, Lamponi S, De Luca F, Novellino E, Campiani G, Docquier JD, Butini S.

J Enzyme Inhib Med Chem. 2016;31(sup1):98-109. Epub 2016 Apr 28.


Verbascoside Inhibits Promastigote Growth and Arginase Activity of Leishmania amazonensis.

Maquiaveli CC, Lucon-Júnior JF, Brogi S, Campiani G, Gemma S, Vieira PC, Silva ER.

J Nat Prod. 2016 May 27;79(5):1459-63. doi: 10.1021/acs.jnatprod.5b00875. Epub 2016 Apr 20.


Development and Pharmacological Characterization of Selective Blockers of 2-Arachidonoyl Glycerol Degradation with Efficacy in Rodent Models of Multiple Sclerosis and Pain.

Brindisi M, Maramai S, Gemma S, Brogi S, Grillo A, Di Cesare Mannelli L, Gabellieri E, Lamponi S, Saponara S, Gorelli B, Tedesco D, Bonfiglio T, Landry C, Jung KM, Armirotti A, Luongo L, Ligresti A, Piscitelli F, Bertucci C, Dehouck MP, Campiani G, Maione S, Ghelardini C, Pittaluga A, Piomelli D, Di Marzo V, Butini S.

J Med Chem. 2016 Mar 24;59(6):2612-32. doi: 10.1021/acs.jmedchem.5b01812. Epub 2016 Mar 7.


The novel pyrrolo-1,5-benzoxazepine, PBOX-15, synergistically enhances the apoptotic efficacy of imatinib in gastrointestinal stromal tumours; suggested mechanism of action of PBOX-15.

Kinsella P, Greene LM, Bright SA, Pollock JK, Butini S, Campiani G, Bauer S, Williams DC, Zisterer DM.

Invest New Drugs. 2016 Apr;34(2):159-67. doi: 10.1007/s10637-016-0331-1. Epub 2016 Feb 17.


In silico study of subtilisin-like protease 1 (SUB1) from different Plasmodium species in complex with peptidyl-difluorostatones and characterization of potent pan-SUB1 inhibitors.

Brogi S, Giovani S, Brindisi M, Gemma S, Novellino E, Campiani G, Blackman MJ, Butini S.

J Mol Graph Model. 2016 Mar;64:121-130. doi: 10.1016/j.jmgm.2016.01.005. Epub 2016 Jan 19.


Multitarget compounds bearing tacrine- and donepezil-like structural and functional motifs for the potential treatment of Alzheimer's disease.

Ismaili L, Refouvelet B, Benchekroun M, Brogi S, Brindisi M, Gemma S, Campiani G, Filipic S, Agbaba D, Esteban G, Unzeta M, Nikolic K, Butini S, Marco-Contelles J.

Prog Neurobiol. 2017 Apr;151:4-34. doi: 10.1016/j.pneurobio.2015.12.003. Epub 2016 Jan 18. Review.


Donepezil-like multifunctional agents: Design, synthesis, molecular modeling and biological evaluation.

Wu MY, Esteban G, Brogi S, Shionoya M, Wang L, Campiani G, Unzeta M, Inokuchi T, Butini S, Marco-Contelles J.

Eur J Med Chem. 2016 Oct 4;121:864-879. doi: 10.1016/j.ejmech.2015.10.001. Epub 2015 Oct 9.


Exploring clotrimazole-based pharmacophore: 3D-QSAR studies and synthesis of novel antiplasmodial agents.

Brogi S, Brindisi M, Joshi BP, Sanna Coccone S, Parapini S, Basilico N, Novellino E, Campiani G, Gemma S, Butini S.

Bioorg Med Chem Lett. 2015 Nov 15;25(22):5412-8. doi: 10.1016/j.bmcl.2015.09.007. Epub 2015 Sep 5.


Antitumor effect of pyrrolo-1,5-benzoxazepine-15 and its synergistic effect with Oxaliplatin and 5-FU in colorectal cancer cells.

Fiore D, Proto MC, Pisanti S, Picardi P, Pagano Zottola AC, Butini S, Gemma S, Casagni A, Laezza C, Vitale M, Ligresti A, Di Marzo V, Zisterer DM, Nathwani S, Williams DC, Campiani G, Gazzerro P, Bifulco M.

Cancer Biol Ther. 2016 Aug 2;17(8):849-58. doi: 10.1080/15384047.2015.1078028.


Endocannabinoid Modulation of Predator Stress-Induced Long-Term Anxiety in Rats.

Lim J, Igarashi M, Jung KM, Butini S, Campiani G, Piomelli D.

Neuropsychopharmacology. 2016 Apr;41(5):1329-39. doi: 10.1038/npp.2015.284. Epub 2015 Sep 11.


Unconventional Knoevenagel-type indoles: Synthesis and cell-based studies for the identification of pro-apoptotic agents.

Spallarossa A, Caneva C, Caviglia M, Alfei S, Butini S, Campiani G, Gemma S, Brindisi M, Zisterer DM, Bright SA, Williams CD, Crespan E, Maga G, Sanna G, Delogu I, Collu G, Loddo R.

Eur J Med Chem. 2015 Sep 18;102:648-60. doi: 10.1016/j.ejmech.2015.08.009. Epub 2015 Aug 8.


Site-directed Mutagenesis of Key Residues Unveiled a Novel Allosteric Site on Human Adenosine Kinase for Pyrrolobenzoxa(thia)zepinone Non-Nucleoside Inhibitors.

Savi L, Brindisi M, Alfano G, Butini S, La Pietra V, Novellino E, Marinelli L, Lossani A, Focher F, Cavella C, Campiani G, Gemma S.

Chem Biol Drug Des. 2016 Jan;87(1):112-20. doi: 10.1111/cbdd.12630. Epub 2015 Sep 18.


Induction of apoptosis in oral squamous carcinoma cells by pyrrolo-1,5-benzoxazepines.

O'Callaghan K, Palagano E, Butini S, Campiani G, Williams DC, Zisterer DM, O'Sullivan J.

Mol Med Rep. 2015 Sep;12(3):3748-3754. doi: 10.3892/mmr.2015.3832. Epub 2015 May 25.


Structure-based discovery of the first non-covalent inhibitors of Leishmania major tryparedoxin peroxidase by high throughput docking.

Brindisi M, Brogi S, Relitti N, Vallone A, Butini S, Gemma S, Novellino E, Colotti G, Angiulli G, Di Chiaro F, Fiorillo A, Ilari A, Campiani G.

Sci Rep. 2015 May 7;5:9705. doi: 10.1038/srep09705.


Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies.

Brindisi M, Butini S, Franceschini S, Brogi S, Trotta F, Ros S, Cagnotto A, Salmona M, Casagni A, Andreassi M, Saponara S, Gorelli B, Weikop P, Mikkelsen JD, Scheel-Kruger J, Sandager-Nielsen K, Novellino E, Campiani G, Gemma S.

J Med Chem. 2014 Nov 26;57(22):9578-97. doi: 10.1021/jm501119j. Epub 2014 Nov 7.


The web of clinical data.

Gori M, Campiani G, Rossi A, Setacci C.

J Cardiovasc Surg (Torino). 2014 Oct;55(5):717-8. No abstract available.


Disease-modifying anti-Alzheimer's drugs: inhibitors of human cholinesterases interfering with β-amyloid aggregation.

Brogi S, Butini S, Maramai S, Colombo R, Verga L, Lanni C, De Lorenzi E, Lamponi S, Andreassi M, Bartolini M, Andrisano V, Novellino E, Campiani G, Brindisi M, Gemma S.

CNS Neurosci Ther. 2014 Jul;20(7):624-32. doi: 10.1111/cns.12290.


Rational design of the first difluorostatone-based PfSUB1 inhibitors.

Giovani S, Penzo M, Brogi S, Brindisi M, Gemma S, Novellino E, Savini L, Blackman MJ, Campiani G, Butini S.

Bioorg Med Chem Lett. 2014 Aug 1;24(15):3582-6. doi: 10.1016/j.bmcl.2014.05.044. Epub 2014 May 23.


Multifunctional cholinesterase and amyloid Beta fibrillization modulators. Synthesis and biological investigation.

Butini S, Brindisi M, Brogi S, Maramai S, Guarino E, Panico A, Saxena A, Chauhan V, Colombo R, Verga L, De Lorenzi E, Bartolini M, Andrisano V, Novellino E, Campiani G, Gemma S.

ACS Med Chem Lett. 2013 Oct 6;4(12):1178-82. doi: 10.1021/ml4002908. eCollection 2013 Dec 12.


Synthesis and structure-activity relationship studies in serotonin 5-HT4 receptor ligands based on a benzo[de][2,6]naphthridine scaffold.

Castriconi F, Paolino M, Giuliani G, Anzini M, Campiani G, Mennuni L, Sabatini C, Lanza M, Caselli G, De Rienzo F, Menziani MC, Sbraccia M, Molinari P, Costa T, Cappelli A.

Eur J Med Chem. 2014 Jul 23;82:36-46. doi: 10.1016/j.ejmech.2014.05.015. Epub 2014 May 5.


The novel pyrrolo-1,5-benzoxazepine, PBOX-6, synergistically enhances the apoptotic effects of carboplatin in drug sensitive and multidrug resistant neuroblastoma cells.

Lennon JC, Bright SA, Carroll E, Butini S, Campiani G, O'Meara A, Williams DC, Zisterer DM.

Biochem Pharmacol. 2014 Feb 15;87(4):611-24. doi: 10.1016/j.bcp.2013.12.017. Epub 2014 Jan 6.


A stereoselective approach to peptidomimetic BACE1 inhibitors.

Butini S, Gabellieri E, Brindisi M, Giovani S, Maramai S, Kshirsagar G, Guarino E, Brogi S, La Pietra V, Giustiniano M, Marinelli L, Novellino E, Campiani G, Cappelli A, Gemma S.

Eur J Med Chem. 2013;70:233-47. doi: 10.1016/j.ejmech.2013.09.056. Epub 2013 Oct 6.


HCV-targeted antivirals: current status and future challenges.

Gemma S, Brogi S, Novellino E, Campiani G, Maga G, Brindisi M, Butini S.

Curr Pharm Des. 2014;20(21):3445-64. Review.


The structural evolution of β-secretase inhibitors: a focus on the development of small-molecule inhibitors.

Butini S, Brogi S, Novellino E, Campiani G, Ghosh AK, Brindisi M, Gemma S.

Curr Top Med Chem. 2013;13(15):1787-807. Review.


PBOX-15 induces apoptosis and improves the efficacy of oxaliplatin in human colorectal cancer cell lines.

Gangemi G, Gazzerro P, Fiore D, Proto MC, Butini S, Gemma S, Casagni A, Laezza C, Vitale M, Ligresti A, Di Marzo V, Zisterer DM, Nathwani S, Clive Williams D, Campiani G, Bifulco M.

Eur J Pharmacol. 2013 Aug 15;714(1-3):379-87. doi: 10.1016/j.ejphar.2013.07.011. Epub 2013 Jul 16. Retraction in: Eur J Pharmacol. 2014 Apr 5;728:190.


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