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Items: 1 to 50 of 70

1.

Specific targeting of peripheral serotonin 5-HT(3) receptors. Synthesis, biological investigation, and structure-activity relationships.

Morelli E, Gemma S, Budriesi R, Campiani G, Novellino E, Fattorusso C, Catalanotti B, Coccone SS, Ros S, Borrelli G, Persico M, Fiorini I, Nacci V, Ioan P, Chiarini A, Hamon M, Cagnotto A, Mennini T, Fracasso C, Colovic M, Caccia S, Butini S.

J Med Chem. 2009 Jun 11;52(11):3548-62. doi: 10.1021/jm900018b.

PMID:
19425598
2.

Combining 4-aminoquinoline- and clotrimazole-based pharmacophores toward innovative and potent hybrid antimalarials.

Gemma S, Campiani G, Butini S, Joshi BP, Kukreja G, Coccone SS, Bernetti M, Persico M, Nacci V, Fiorini I, Novellino E, Taramelli D, Basilico N, Parapini S, Yardley V, Croft S, Keller-Maerki S, Rottmann M, Brun R, Coletta M, Marini S, Guiso G, Caccia S, Fattorusso C.

J Med Chem. 2009 Jan 22;52(2):502-13. doi: 10.1021/jm801352s.

PMID:
19113955
3.

Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.

Butini S, Gemma S, Campiani G, Franceschini S, Trotta F, Borriello M, Ceres N, Ros S, Coccone SS, Bernetti M, De Angelis M, Brindisi M, Nacci V, Fiorini I, Novellino E, Cagnotto A, Mennini T, Sandager-Nielsen K, Andreasen JT, Scheel-Kruger J, Mikkelsen JD, Fattorusso C.

J Med Chem. 2009 Jan 8;52(1):151-69. doi: 10.1021/jm800689g.

PMID:
19072656
4.

Exploiting protein fluctuations at the active-site gorge of human cholinesterases: further optimization of the design strategy to develop extremely potent inhibitors.

Butini S, Campiani G, Borriello M, Gemma S, Panico A, Persico M, Catalanotti B, Ros S, Brindisi M, Agnusdei M, Fiorini I, Nacci V, Novellino E, Belinskaya T, Saxena A, Fattorusso C.

J Med Chem. 2008 Jun 12;51(11):3154-70. doi: 10.1021/jm701253t. Epub 2008 May 15.

PMID:
18479118
5.

Clotrimazole scaffold as an innovative pharmacophore towards potent antimalarial agents: design, synthesis, and biological and structure-activity relationship studies.

Gemma S, Campiani G, Butini S, Kukreja G, Coccone SS, Joshi BP, Persico M, Nacci V, Fiorini I, Novellino E, Fattorusso E, Taglialatela-Scafati O, Savini L, Taramelli D, Basilico N, Parapini S, Morace G, Yardley V, Croft S, Coletta M, Marini S, Fattorusso C.

J Med Chem. 2008 Mar 13;51(5):1278-94. doi: 10.1021/jm701247k. Epub 2008 Feb 16.

PMID:
18278860
6.

Design, synthesis, and structure-activity relationship studies of 4-quinolinyl- and 9-acrydinylhydrazones as potent antimalarial agents.

Fattorusso C, Campiani G, Kukreja G, Persico M, Butini S, Romano MP, Altarelli M, Ros S, Brindisi M, Savini L, Novellino E, Nacci V, Fattorusso E, Parapini S, Basilico N, Taramelli D, Yardley V, Croft S, Borriello M, Gemma S.

J Med Chem. 2008 Mar 13;51(5):1333-43. doi: 10.1021/jm7012375. Epub 2008 Feb 16.

PMID:
18278859
7.

Design and synthesis of potent antimalarial agents based on clotrimazole scaffold: exploring an innovative pharmacophore.

Gemma S, Campiani G, Butini S, Kukreja G, Joshi BP, Persico M, Catalanotti B, Novellino E, Fattorusso E, Nacci V, Savini L, Taramelli D, Basilico N, Morace G, Yardley V, Fattorusso C.

J Med Chem. 2007 Feb 22;50(4):595-8. Epub 2007 Jan 31.

PMID:
17263523
8.

Discovery of huperzine A-tacrine hybrids as potent inhibitors of human cholinesterases targeting their midgorge recognition sites.

Gemma S, Gabellieri E, Huleatt P, Fattorusso C, Borriello M, Catalanotti B, Butini S, De Angelis M, Novellino E, Nacci V, Belinskaya T, Saxena A, Campiani G.

J Med Chem. 2006 Jun 1;49(11):3421-5.

PMID:
16722663
9.

Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. Design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity.

Fattorusso C, Gemma S, Butini S, Huleatt P, Catalanotti B, Persico M, De Angelis M, Fiorini I, Nacci V, Ramunno A, Rodriquez M, Greco G, Novellino E, Bergamini A, Marini S, Coletta M, Maga G, Spadari S, Campiani G.

J Med Chem. 2005 Nov 17;48(23):7153-65.

PMID:
16279773
10.

The pyrrolo-1,5-benzoxazepine, PBOX-6, inhibits the growth of breast cancer cells in vitro independent of estrogen receptor status and inhibits breast tumour growth in vivo.

Greene LM, Fleeton M, Mulligan J, Gowda C, Sheahan BJ, Atkins GJ, Campiani G, Nacci V, Lawler M, Williams DC, Zisterer DM.

Oncol Rep. 2005 Nov;14(5):1357-63.

PMID:
16211309
11.

Specific targeting of hepatitis C virus NS3 RNA helicase. Discovery of the potent and selective competitive nucleotide-mimicking inhibitor QU663.

Maga G, Gemma S, Fattorusso C, Locatelli GA, Butini S, Persico M, Kukreja G, Romano MP, Chiasserini L, Savini L, Novellino E, Nacci V, Spadari S, Campiani G.

Biochemistry. 2005 Jul 19;44(28):9637-44.

PMID:
16008349
12.

Pyrrolo[1,5]benzoxa(thia)zepines as a new class of potent apoptotic agents. Biological studies and identification of an intracellular location of their drug target.

Mc Gee MM, Gemma S, Butini S, Ramunno A, Zisterer DM, Fattorusso C, Catalanotti B, Kukreja G, Fiorini I, Pisano C, Cucco C, Novellino E, Nacci V, Williams DC, Campiani G.

J Med Chem. 2005 Jun 30;48(13):4367-77.

PMID:
15974589
13.

Development of molecular probes for the identification of extra interaction sites in the mid-gorge and peripheral sites of butyrylcholinesterase (BuChE). Rational design of novel, selective, and highly potent BuChE inhibitors.

Campiani G, Fattorusso C, Butini S, Gaeta A, Agnusdei M, Gemma S, Persico M, Catalanotti B, Savini L, Nacci V, Novellino E, Holloway HW, Greig NH, Belinskaya T, Fedorko JM, Saxena A.

J Med Chem. 2005 Mar 24;48(6):1919-29.

PMID:
15771436
14.

Novel atypical antipsychotic agents: rational design, an efficient palladium-catalyzed route, and pharmacological studies.

Campiani G, Butini S, Fattorusso C, Trotta F, Gemma S, Catalanotti B, Nacci V, Fiorini I, Cagnotto A, Mereghetti I, Mennini T, Minetti P, Di Cesare MA, Stasi MA, Di Serio S, Ghirardi O, Tinti O, Carminati P.

J Med Chem. 2005 Mar 24;48(6):1705-8.

PMID:
15771414
16.

Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents.

Campiani G, Butini S, Fattorusso C, Catalanotti B, Gemma S, Nacci V, Morelli E, Cagnotto A, Mereghetti I, Mennini T, Carli M, Minetti P, Di Cesare MA, Mastroianni D, Scafetta N, Galletti B, Stasi MA, Castorina M, Pacifici L, Vertechy M, Di Serio S, Ghirardi O, Tinti O, Carminati P.

J Med Chem. 2004 Jan 1;47(1):143-57.

PMID:
14695828
17.

Inhibition of G1 cyclin-dependent kinase activity during growth arrest of human astrocytoma cells by the pyrrolo-1,5-benzoxazepine, PBOX-21.

Mulligan JM, Campiani G, Ramunno A, Nacci V, Zisterer DM.

Biochim Biophys Acta. 2003 Sep 1;1639(1):43-52.

18.

Synthesis and pharmacological evaluation of potent and highly selective D3 receptor ligands: inhibition of cocaine-seeking behavior and the role of dopamine D3/D2 receptors.

Campiani G, Butini S, Trotta F, Fattorusso C, Catalanotti B, Aiello F, Gemma S, Nacci V, Novellino E, Stark JA, Cagnotto A, Fumagalli E, Carnovali F, Cervo L, Mennini T.

J Med Chem. 2003 Aug 28;46(18):3822-39.

PMID:
12930145
19.

Neuronal high-affinity sodium-dependent glutamate transporters (EAATs): targets for the development of novel therapeutics against neurodegenerative diseases.

Campiani G, Fattorusso C, De Angelis M, Catalanotti B, Butini S, Fattorusso R, Fiorini I, Nacci V, Novellino E.

Curr Pharm Des. 2003;9(8):599-625. Review.

PMID:
12570795
20.

Synthesis of new molecular probes for investigation of steroid biosynthesis induced by selective interaction with peripheral type benzodiazepine receptors (PBR).

Campiani G, Ramunno A, Fiorini I, Nacci V, Morelli E, Novellino E, Goegan M, Mennini T, Sullivan S, Zisterer DM, Williams CD.

J Med Chem. 2002 Sep 12;45(19):4276-81.

PMID:
12213069
21.

Non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors: past, present, and future perspectives.

Campiani G, Ramunno A, Maga G, Nacci V, Fattorusso C, Catalanotti B, Morelli E, Novellino E.

Curr Pharm Des. 2002;8(8):615-57. Review.

PMID:
11945162
22.

Caspase-3 is not essential for DNA fragmentation in MCF-7 cells during apoptosis induced by the pyrrolo-1,5-benzoxazepine, PBOX-6.

Mc Gee MM, Hyland E, Campiani G, Ramunno A, Nacci V, Zisterer DM.

FEBS Lett. 2002 Mar 27;515(1-3):66-70.

23.

Activation of the c-Jun N-terminal kinase (JNK) signaling pathway is essential during PBOX-6-induced apoptosis in chronic myelogenous leukemia (CML) cells.

Mc Gee MM, Campiani G, Ramunno A, Nacci V, Lawler M, Williams DC, Zisterer DM.

J Biol Chem. 2002 May 24;277(21):18383-9. Epub 2002 Feb 20.

24.

Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.

Campiani G, Butini S, Gemma S, Nacci V, Fattorusso C, Catalanotti B, Giorgi G, Cagnotto A, Goegan M, Mennini T, Minetti P, Di Cesare MA, Mastroianni D, Scafetta N, Galletti B, Stasi MA, Castorina M, Pacifici L, Ghirardi O, Tinti O, Carminati P.

J Med Chem. 2002 Jan 17;45(2):344-59.

PMID:
11784139
25.

Pyrrolo-1,5-Benzoxazepines Induce Apoptosis in Chronic Myeloid Leukemia (CML) Cells by Bypassing the Apoptotic Suppressor BCR-ABL.

Mc Gee MM, Campiani G, Ramunno A, Fattorusso C, Nacci V, Lawler M, Williams DC, Zisterer DM.

ScientificWorldJournal. 2001 Dec 19;1:109. doi: 10.1100/tsw.2001.122. eCollection 2001. No abstract available.

26.

Characterization of the 1H-cyclopentapyrimidine-2,4(1H,3H)-dione derivative (S)-CPW399 as a novel, potent, and subtype-selective AMPA receptor full agonist with partial desensitization properties.

Campiani G, Morelli E, Nacci V, Fattorusso C, Ramunno A, Novellino E, Greenwood J, Liljefors T, Griffiths R, Sinclair C, Reavy H, Kristensen AS, Pickering DS, Schousboe A, Cagnotto A, Fumagalli E, Mennini T.

J Med Chem. 2001 Dec 20;44(26):4501-4.

PMID:
11741469
27.

Pyrrolo-1,5-benzoxazepines: a new class of apoptotic agents.

Zisterer DM, McGee MM, Campiani G, Ramunno A, Fattorusso C, Nacci V, Lawler M, Williams DC.

Biochem Soc Trans. 2001 Nov;29(Pt 6):704-6.

PMID:
11709059
28.

The stereoselective targeting of a specific enzyme-substrate complex is the molecular mechanism for the synergic inhibition of HIV-1 reverse transcriptase by (R)-(-)-PPO464: a novel generation of nonnucleoside inhibitors.

Maga G, Ramunno A, Nacci V, Locatelli GA, Spadari S, Fiorini I, Baldanti F, Paolucci S, Zavattoni M, Bergamini A, Galletti B, Muck S, Hubscher U, Giorgi G, Guiso G, Caccia S, Campiani G.

J Biol Chem. 2001 Nov 30;276(48):44653-62. Epub 2001 Sep 25.

29.

A rational approach to the design of selective substrates and potent nontransportable inhibitors of the excitatory amino acid transporter EAAC1 (EAAT3). new glutamate and aspartate analogues as potential neuroprotective agents.

Campiani G, De Angelis M, Armaroli S, Fattorusso C, Catalanotti B, Ramunno A, Nacci V, Novellino E, Grewer C, Ionescu D, Rauen T, Griffiths R, Sinclair C, Fumagalli E, Mennini T.

J Med Chem. 2001 Aug 2;44(16):2507-10. No abstract available.

PMID:
11472204
30.

Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent.

Campiani G, Aiello F, Fabbrini M, Morelli E, Ramunno A, Armaroli S, Nacci V, Garofalo A, Greco G, Novellino E, Maga G, Spadari S, Bergamini A, Ventura L, Bongiovanni B, Capozzi M, Bolacchi F, Marini S, Coletta M, Guiso G, Caccia S.

J Med Chem. 2001 Feb 1;44(3):305-15.

PMID:
11462972
31.

Pyrrolo-1,5-benzoxazepines induce apoptosis in chronic myelogenous leukemia (CML) cells by bypassing the apoptotic suppressor bcr-abl.

Mc Gee MM, Campiani G, Ramunno A, Fattorusso C, Nacci V, Lawler M, Williams DC, Zisterer DM.

J Pharmacol Exp Ther. 2001 Jan;296(1):31-40.

PMID:
11123359
32.

Non-nucleoside HIV-1 reverse transcriptase inhibitors: synthesis and biological evaluation of novel quinoxalinylethylpyridylthioureas as potent antiviral agents.

Campiani G, Fabbrini M, Morelli E, Nacci V, Greco G, Novellino E, Maga G, Spadari S, Bergamini A, Faggioli E, Uccella I, Bolacchi F, Marini S, Coletta M, Fracasso C, Caccia S.

Antivir Chem Chemother. 2000 Mar;11(2):141-55.

PMID:
10819438
33.

Pyrrolo-1,5-benzoxazepines induce apoptosis in HL-60, Jurkat, and Hut-78 cells: a new class of apoptotic agents.

Zisterer DM, Campiani G, Nacci V, Williams DC.

J Pharmacol Exp Ther. 2000 Apr;293(1):48-59.

PMID:
10734152
34.

Pyrrolobenzoxazepinone derivatives as non-nucleoside HIV-1 RT inhibitors: further structure-activity relationship studies and identification of more potent broad-spectrum HIV-1 RT inhibitors with antiviral activity.

Campiani G, Morelli E, Fabbrini M, Nacci V, Greco G, Novellino E, Ramunno A, Maga G, Spadari S, Caliendo G, Bergamini A, Faggioli E, Uccella I, Bolacchi F, Marini S, Coletta M, Nacca A, Caccia S.

J Med Chem. 1999 Oct 21;42(21):4462-70.

PMID:
10543890
35.

Pyrroloquinoxaline derivatives as high-affinity and selective 5-HT(3) receptor agonists: synthesis, further structure-activity relationships, and biological studies.

Campiani G, Morelli E, Gemma S, Nacci V, Butini S, Hamon M, Novellino E, Greco G, Cagnotto A, Goegan M, Cervo L, Dalla Valle F, Fracasso C, Caccia S, Mennini T.

J Med Chem. 1999 Oct 21;42(21):4362-79.

PMID:
10543880
36.

Thiazolothiazepine inhibitors of HIV-1 integrase.

Neamati N, Turpin JA, Winslow HE, Christensen JL, Williamson K, Orr A, Rice WG, Pommier Y, Garofalo A, Brizzi A, Campiani G, Fiorini I, Nacci V.

J Med Chem. 1999 Aug 26;42(17):3334-41.

PMID:
10464020
37.

Synthesis and anticholinesterase activity of huperzine A analogues containing phenol and catechol replacements for the pyridone ring.

Campiani G, Kozikowski AP, Wang S, Ming L, Nacci V, Saxena A, Doctor BP.

Bioorg Med Chem Lett. 1998 Jun 2;8(11):1413-8.

PMID:
9871776
38.

New antipsychotic agents with serotonin and dopamine antagonist properties based on a pyrrolo[2,1-b][1,3]benzothiazepine structure.

Campiani G, Nacci V, Bechelli S, Ciani SM, Garofalo A, Fiorini I, Wikström H, de Boer P, Liao Y, Tepper PG, Cagnotto A, Mennini T.

J Med Chem. 1998 Sep 24;41(20):3763-72.

PMID:
9748351
39.

Antiproliferative action of pyrrolobenzoxazepine derivatives in cultured cells: absence of correlation with binding to the peripheral-type benzodiazepine binding site.

Zisterer DM, Hance N, Campiani G, Garofalo A, Nacci V, Williams DC.

Biochem Pharmacol. 1998 Feb 15;55(4):397-403.

PMID:
9514073
40.

Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure.

Campiani G, Cappelli A, Nacci V, Anzini M, Vomero S, Hamon M, Cagnotto A, Fracasso C, Uboldi C, Caccia S, Consolo S, Mennini T.

J Med Chem. 1997 Oct 24;40(22):3670-8.

PMID:
9357534
41.

Diltiazem-like calcium entry blockers: a hypothesis of the receptor-binding site based on a comparative molecular field analysis model.

Corelli F, Manetti F, Tafi A, Campiani G, Nacci V, Botta M.

J Med Chem. 1997 Jan 3;40(1):125-31.

PMID:
9016337
42.

Synthesis, biological activity, and SARs of pyrrolobenzoxazepine derivatives, a new class of specific "peripheral-type" benzodiazepine receptor ligands.

Campiani G, Nacci V, Fiorini I, De Filippis MP, Garofalo A, Ciani SM, Greco G, Novellino E, Williams DC, Zisterer DM, Woods MJ, Mihai C, Manzoni C, Mennini T.

J Med Chem. 1996 Aug 30;39(18):3435-50.

PMID:
8784441
43.

Cardiovascular characterization of pyrrolo[2,1-d][1,5]benzothiazepine derivatives binding selectively to the peripheral-type benzodiazepine receptor (PBR): from dual PBR affinity and calcium antagonist activity to novel and selective calcium entry blockers.

Campiani G, Fiorini I, De Filippis MP, Ciani SM, Garofalo A, Nacci V, Giorgi G, Sega A, Botta M, Chiarini A, Budriesi R, Bruni G, Romeo MR, Manzoni C, Mennini T.

J Med Chem. 1996 Jul 19;39(15):2922-38.

PMID:
8709127
44.

Pyrrolobenzothiazepinones and pyrrolobenzoxazepinones: novel and specific non-nucleoside HIV-1 reverse transcriptase inhibitors with antiviral activity.

Campiani G, Nacci V, Fiorini I, De Filippis MP, Garofalo A, Greco G, Novellino E, Altamura S, Di Renzo L.

J Med Chem. 1996 Jul 5;39(14):2672-80.

PMID:
8709096
45.
46.

Pyrrolo[2,1-c][1,4]benzothiazines: synthesis, structure-activity relationships, molecular modeling studies, and cardiovascular activity.

Campiani G, Garofalo A, Fiorini I, Botta M, Nacci V, Tafi A, Chiarini A, Budriesi R, Bruni G, Romeo MR.

J Med Chem. 1995 Oct 27;38(22):4393-410.

PMID:
7473567
47.

A comparative molecular field analysis model for 6-arylpyrrolo[2,1-d] [1,5]benzothiazepines binding selectively to the mitochondrial benzodiazepine receptor.

Greco G, Novellino E, Fiorini I, Nacci V, Campiani G, Ciani SM, Garofalo A, Bernasconi P, Mennini T.

J Med Chem. 1994 Nov 25;37(24):4100-8.

PMID:
7990110
48.

Novel ligands specific for mitochondrial benzodiazepine receptors: 6-arylpyrrolo[2,1-d][1,5]benzothiazepine derivatives. Synthesis, structure-activity relationships, and molecular modeling studies.

Fiorini I, Nacci V, Ciani SM, Garofalo A, Campiani G, Savini L, Novellino E, Greco G, Bernasconi P, Mennini T.

J Med Chem. 1994 May 13;37(10):1427-38.

PMID:
8182701
49.

Benzothiazine and benzothiazepine derivatives: synthesis and preliminary biological evaluation.

Garofalo A, Campiani G, Fiorini I, Nacci V.

Farmaco. 1993 Feb;48(2):275-83.

PMID:
8494599

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