Research Topics
| G CampianiSummaryAffiliation: University of Siena Country: Italy Publications
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Detail Information
Publications
Synthesis of N1-arylidene-N2-quinolyl- and N2-acrydinylhydrazones as potent antimalarial agents active against CQ-resistant P. falciparum strainsSandra Gemma
Dipartimento Farmaco Chimico Tecnologico, , Via Aldo Moro, 53100 Siena, Italy
Bioorg Med Chem Lett 16:5384-8. 2006..These compounds showed remarkable anti-plasmodial activity in vitro especially against chloroquine-resistant strains. Their potent biological activity makes them promising lead structures for the development of new antimalarial drugs...- STI-571 (imatinib mesylate) enhances the apoptotic efficacy of pyrrolo-1,5-benzoxazepine-6, a novel microtubule-targeting agent, in both STI-571-sensitive and -resistant Bcr-Abl-positive human chronic myeloid leukemia cellsLisa M Greene
School of Biochemistry and Immunology, Trinity College, Dublin 2, United Kingdom
J Pharmacol Exp Ther 321:288-97. 2007..Together, these findings highlight the potential clinical benefits in simultaneously targeting the microtubules and the Bcr-Abl oncoprotein in STI-571-sensitive and -resistant CML cells... 
Broad inhibition of plasmodium falciparum cytoadherence by (+)-epigallocatechin gallatePradeep R Patil
European Research Centre for Drug Discovery and Development, Department of Pharmaceutical and Applied Chemistry, University of Siena, Italy
Malar J 10:348. 2011..Here, this property is further explored using a new panel of ICAM-1-binding patient isolates of P. falciparum to ascertain if (+)-EGCG might be effective as a broad spectrum inhibitor of ICAM-1-based cytoadherence...- 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 propertiesG Campiani
Dipartimento Farmaco Chimico Tecnologico DFCT, Universita degli Studi di Siena, Via Aldo Moro, 53100 Siena, Italy
J Med Chem 44:4501-4. 2001.... - Synthesis of new molecular probes for investigation of steroid biosynthesis induced by selective interaction with peripheral type benzodiazepine receptors (PBR)Giuseppe Campiani
Dipartimento Farmaco Chimico Tecnologico, Universita degli Studi di Siena, Via Aldo Moro, 53100 Siena, Italy
J Med Chem 45:4276-81. 2002..Several compounds, differently substituted at C-7, were used as molecular yardsticks to probe the spatial dimension of the lipophilic pocket L4 in the receptor binding site... - Neuronal high-affinity sodium-dependent glutamate transporters (EAATs): targets for the development of novel therapeutics against neurodegenerative diseasesGiuseppe Campiani
Dipartimento Farmaco Chimico Tecnologico DFCT, Universita degli Studi di Siena, Via Aldo Moro, 53100 Siena, Italy
Curr Pharm Des 9:599-625. 2003.... - Synthesis and pharmacological evaluation of potent and highly selective D3 receptor ligands: inhibition of cocaine-seeking behavior and the role of dopamine D3/D2 receptorsGiuseppe Campiani
Dipartimento Farmaco Chimico Tecnologico, Universita di Siena, Via Aldo Moro, 53100 Siena, Italy
J Med Chem 46:3822-39. 2003.... - Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agentsGiuseppe Campiani
Dipartimento Farmaco Chimico Tecnologico, Via Aldo Moro and European Research Centre for Drug Discovery and Development, Universita degli Studi di Siena, 53100 Siena, Italy
J Med Chem 47:143-57. 2004..In conclusion, the pharmacological profile of 9d proved better than clozapine and olanzapine, making this compound a potential clinical candidate... - Novel atypical antipsychotic agents: rational design, an efficient palladium-catalyzed route, and pharmacological studiesGiuseppe Campiani
Dipartimento Farmaco Chimico Tecnologico, Via Aldo Moro, and European Research Centre for Drug Discovery and Development, Universita di Siena, 53100 Siena, Italy
J Med Chem 48:1705-8. 2005..5a was active on conditioned avoidance response at 0.56 mg/kg, it had low cataleptic potential and proved to be better than ST1899, clozapine, and olanzapine, representing a new clinical candidate... - 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 inhibitorsGiuseppe Campiani
Dipartimento Farmaco Chimico Tecnologico, Via Aldo Moro, and European Research Centre for Drug Discovery and Development NatSynDrugs, Universita di Siena, 53100 Siena, Italy
J Med Chem 48:1919-29. 2005..The novel inhibitors, bearing postulated key features, validated the hypothesis of the presence of extra interaction sites within the hBuChE active site gorge... 
Design, synthesis, and structure-activity relationship studies of 4-quinolinyl- and 9-acrydinylhydrazones as potent antimalarial agentsCaterina Fattorusso
J Med Chem 51:1333-43. 2008..The mechanism of action of the novel compounds was investigated and their in vivo activity was assessed...- Non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors: past, present, and future perspectivesGiuseppe Campiani
Dipartimento Farmaco Chimico Tecnologico, Universita degli Studi di Siena, Via Aldo Moro, 53100 Siena, Italy
Curr Pharm Des 8:615-57. 2002..Starting from the first generation, this review will focus on the second generation NNRTIs dealing with the recent and most interesting published results, highlighting the guidelines for the development of a third generation of NNRTIs... - Pyrroloquinoxaline derivatives as high-affinity and selective 5-HT(3) receptor agonists: synthesis, further structure-activity relationships, and biological studiesG Campiani
Dipartimento di Scienze Farmaceutiche, Facolta di Farmacia, Universita degli Studi di Salerno, Via Ponte Don Melillo, 84084 Fisciano, Salerno, Italy
J Med Chem 42:4362-79. 1999..None of the tested compounds showed in vivo anxiolytic-like activity, but potential analgesic-like properties have been possibly disclosed for this new class of 5-HT(3) receptor agonists... - Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studiesGiuseppe Campiani
Dipartimento Farmaco Chimico Tecnologico, Universita degli Studi di Siena, Via Aldo Moro, 53100 Siena, Italy
J Med Chem 45:344-59. 2002..The molecular structure determination of the enantiomers of 5 by X-ray diffraction and molecular modeling is reported... - 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 activityG Campiani
Dipartimento di Scienze Farmaceutiche, Facolta di Farmacia, Universita degli Studi di Salerno, Via Ponte Don Melillo, 84084 Fisciano SA, Italy
J Med Chem 42:4462-70. 1999.... - Non-nucleoside HIV-1 reverse transcriptase inhibitors: synthesis and biological evaluation of novel quinoxalinylethylpyridylthioureas as potent antiviral agentsG Campiani
Dipartimento di Scienze Farmaceutiche, Facolta di Farmacia, Universita degli Studi di Salerno, Fisciano Salerno, Italy
Antivir Chem Chemother 11:141-55. 2000..Moreover, 6-FQXPT showed synergistic antiviral activity with zidovudine... - 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 agentG Campiani
Dipartimento di Scienze Farmaceutiche, Facolta di Farmacia, Universita degli Studi di Salerno, Fisciano, Italy
J Med Chem 44:305-15. 2001..Replacing the ethylthioureidic moiety with a hydrazine linker led to a new antiviral lead, offering promising pharmacological and pharmacokinetic properties in terms of antiviral activity and oral bioavailability... - Specific targeting of acetylcholinesterase and butyrylcholinesterase recognition sites. Rational design of novel, selective, and highly potent cholinesterase inhibitorsLuisa Savini
Dipartimento Farmaco Chimico Tecnologico, , Via Aldo Moro, 53100 Siena, Italy
J Med Chem 46:1-4. 2003..The nitrogen-containing homobivalent ligands 3e,g and the sulfur-containing 3h validated the hypothesis of extra sites of interaction in the AChE and BuChE active site gorges... - Development of piperazine-tethered heterodimers as potent antimalarials against chloroquine-resistant P. falciparum strains. Synthesis and molecular modelingSandra Gemma
European Research Centre for Drug Discovery and Development, Universita di Siena, Via Aldo Moro, 53100 Siena, Italy
Bioorg Med Chem Lett 17:3535-9. 2007..Computational studies revealed that the activity is likely due to the ability of the compounds to assume a multisite iron coordinating geometry... - Exploiting protein fluctuations at the active-site gorge of human cholinesterases: further optimization of the design strategy to develop extremely potent inhibitorsStefania Butini
European Research Centre for Drug Discovery and Development NatSynDrugs, Universita di Siena, Siena, Italy
J Med Chem 51:3154-70. 2008..A number of SAR trends were identified, and the multisite inhibitors 3a and 3d were found to be the most potent inhibitors of hBuChE and hAChE known to date... - Discovery of huperzine A-tacrine hybrids as potent inhibitors of human cholinesterases targeting their midgorge recognition sitesSandra Gemma
Dipartimento Farmaco Chimico Tecnologico, Via Aldo Moro, Universita' di Siena, 53100 Siena, Italy
J Med Chem 49:3421-5. 2006..Compounds 5a-c show a markedly improved biological profile relative to tacrine and huperzine A... - Tacrine based human cholinesterase inhibitors: synthesis of peptidic-tethered derivatives and their effect on potency and selectivityStefania Butini
European Research Centre for Drug Discovery and Development NatSynDrugs, Via Aldo Moro 2, 53100 Siena, Italy
Bioorg Med Chem Lett 18:5213-6. 2008..Analogues 3i,j and 3l,m were identified as promising hits and may pave the way for the development of a new series of tacrine based enzyme selective hChEIs... - Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutationsStefania Butini
Dipartimento Farmaco Chimico Tecnologico, Universita di Siena, Via Aldo Moro 2, 53100 Siena, Italy
J Med Chem 52:1224-8. 2009..For the novel compounds (S)-(+)-5 and (S)-(-)-7, a clear-cut stereoselective mechanism of enzyme inhibition was found. Molecular modeling studies were performed for revealing the underpinnings of this behavior... - Novel and potent tacrine-related hetero- and homobivalent ligands for acetylcholinesterase and butyrylcholinesteraseL Savini
Dipartimento Farmaco Chimico Tecnologico, Universita degli Studi di Siena, Via Aldo Moro, 53100, Siena, Italy
Bioorg Med Chem Lett 11:1779-82. 2001..The syntheses of these materials together with the results of AChE/BuChE inhibition assays are detailed... - Diltiazem-like calcium entry blockers: a hypothesis of the receptor-binding site based on a comparative molecular field analysis modelF Corelli
Dipartimento Farmaco Chimico Tecnologico, Universita degli Studi di Siena, Italy
J Med Chem 40:125-31. 1997.... - The interactions of the 5-HT3 receptor with quipazine-like arylpiperazine ligands: the journey track at the end of the first decade of the third millenniumAndrea Cappelli
Dipartimento Farmaco Chimico Tecnologico and European Research Centre for Drug Discovery and Development, Universita di Siena, Via A Moro, 53100 Siena, Italy
Curr Top Med Chem 10:504-26. 2010..The discussion is focused mainly on the most significant structure-affinity relationships emerged in the progress of the work and shows how the original ideas have evolved in the recent years... - 1H-cyclopentapyrimidine-2,4(1H,3H)-dione-related ionotropic glutamate receptors ligands. structure-activity relationships and identification of potent and Selective iGluR5 modulatorsStefania Butini
European Research Centre for Drug Discovery and Development NatSynDrugs, Banchi di Sotto 55, 53100 Siena, Italy
J Med Chem 51:6614-8. 2008.... - Discovery of bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptorsStefania Butini
European Research Centre for Drug Discovery and Development, Universita di Siena, 53100 Siena, Italy
J Med Chem 53:4803-7. 2010.... - Design and synthesis of potent antimalarial agents based on clotrimazole scaffold: exploring an innovative pharmacophoreSandra Gemma
Dipartimento Farmaco Chimico Tecnologico and European Research Centre for Drug Discovery and Development, Universita di Siena, Via Aldo Moro, 53100 Siena, Italy
J Med Chem 50:595-8. 2007..This study allowed us to discover compounds characterized by a high in vitro potency, particularly against Pf CQ-resistant strains selectively targeting free heme, which are easy to synthesize by low-cost synthetic strategies... - Novel, potent, and selective quinoxaline-based 5-HT(3) receptor ligands. 1. Further structure-activity relationships and pharmacological characterizationStefania Butini
European Research Centre for Drug Discovery and Development, 53100 Siena, Italy
J Med Chem 52:6946-50. 2009..In von Bezold-Jarisch reflex test 3a-c were partial agonists while 3i was a full agonist. Preliminary pharmacokinetic studies indicated that 3a is a brain penetrating agent... - Development of antitubercular compounds based on a 4-quinolylhydrazone scaffold. Further structure-activity relationship studiesSandra Gemma
European Research Centre for Drug Discovery and Development, Universita di Siena, Italy
Bioorg Med Chem 17:6063-72. 2009..Further screening allowed the identification of very potent antitubercular agents. Compound 4c was also tested in a time-course experiment and against mtb clinical isolates, displaying interesting results... - Synthesis of dihydroplakortin, 6-epi-dihydroplakortin, and their C10-desethyl analoguesSandra Gemma
Dipartimento Farmaco Chimico Tecnologico DFCT, University of Siena, Via Aldo Moro 2, 53100 Siena, Italy
J Org Chem 75:2333-40. 2010..Homologation of the aldehyde resulting from diol cleavage through a Wittig-based strategy gave access to the ester-containing lateral chain at C3... - An efficient approach to chiral C8/C9-piperazino-substituted 1,4-benzodiazepin-2-ones as peptidomimetic scaffoldsStefania Butini
European Research Centre for Drug Discovery and Development NatSynDrugs, University of Siena, Banchi di Sotto 55, 53100 Siena, Italy
J Org Chem 73:8458-68. 2008.... - Pyrroloquinoxaline hydrazones as fluorescent probes for amyloid fibrilsSandra Gemma
European Research Centre for Drug Discovery and Development NatSynDrugs, University of Siena, Via Aldo Moro, 53100, Siena, Italy
Org Biomol Chem 9:5137-48. 2011..Moreover, their experimentally proven ability to cross the blood-brain barrier in mouse opens the possibility of developing these compounds as potential amyloid imaging agents for in vivo applications... - Unexpected formation of hydroxybiphenylmethane derivatives and some new observations on Labat testGagan Kukreja
Dipartimento Farmaco Chimico Tecnologico, Via Aldo Moro, and European Research Centre for Drug Discovery and Development, Universita di Siena, 53100 Siena, Italy
Nat Prod Res 20:1150-4. 2006..Some new interesting observations of Labat test on colorimetric detection of bichalconyloxy, bichalconyl and biflavonylmethanes having oxygenated ortho positions are presented... - Combining 4-aminoquinoline- and clotrimazole-based pharmacophores toward innovative and potent hybrid antimalarialsSandra Gemma
European Research Centre for Drug Discovery and Development and Dipartimento Farmaco Chimico Tecnologico, Universita di Siena, Via Aldo Moro, 53100 Siena, Italy
J Med Chem 52:502-13. 2009..Among the compounds synthesized, 4g was active in vivo against P. chabaudi and P. berghei after oral administration and, possessing promising pharmacokinetic properties, it is a candidate for further preclinical development... - Tyr702 is an important determinant of agonist binding and domain closure of the ligand-binding core of GluR2Anne Frandsen
Biostructural Research, Department of Medicinal Chemistry, Danish University of Pharmaceutical Sciences, Universitetsparken 2, DK-2100, Copenhagen, Denmark
Mol Pharmacol 67:703-13. 2005..Although it clearly controls selectivity, mutation of this residue alone is insufficient to explain agonist-induced conformational rearrangements occurring in this variant... - Effects of drug resistance mutations L100I and V106A on the binding of pyrrolobenzoxazepinone nonnucleoside inhibitors to the human immunodeficiency virus type 1 reverse transcriptase catalytic complexGiada A Locatelli
Istituto di Genetica Molecolare IGM-CNR, Consiglio Nazionale delle Ricerche, 27100 Pavia, Italy
Antimicrob Agents Chemother 48:1570-80. 2004..This latter mutation also caused a severe reduction in the catalytic efficiency of the RT. These results provide a correlation between the efficiency of nucleotide utilization by RT and its resistance to PBO inhibition... - Identification of tubulin as the molecular target of proapoptotic pyrrolo-1,5-benzoxazepinesJude M Mulligan
School of Biochemistry and Immunology, Trinity College, Dublin 2, Ireland
Mol Pharmacol 70:60-70. 2006..The ability of PBOX-6 to bind tubulin and cause microtubule depolymerization confirms it as a novel candidate for antineoplastic therapy... - 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 targetMargaret M Mc Gee
Department of Biochemistry, Trinity College, Dublin 2, Ireland
J Med Chem 48:4367-77. 2005..Interestingly, compound 6 displayed cytotoxic activity against a panel of human tumor cell lines but demonstrated negligible toxicity in vivo with no effect on the animals' hematology parameters... - Clotrimazole scaffold as an innovative pharmacophore towards potent antimalarial agents: design, synthesis, and biological and structure-activity relationship studiesSandra Gemma
Universita di Siena, Sienna, Italy
J Med Chem 51:1278-94. 2008..Compounds 2, 4e, and 4n exhibited in vivo activity against P. chabaudi after oral administration and thus represent promising antimalarial agents for further preclinical development... - Specific targeting of hepatitis C virus NS3 RNA helicase. Discovery of the potent and selective competitive nucleotide-mimicking inhibitor QU663Giovanni Maga
Istituto di Genetica Molecolare, CNR-Pavia, via Abbiategrasso 207, 27100 Pavia, Italy
Biochemistry 44:9637-44. 2005..A thorough molecular modeling study was carried out to explain the molecular basis of NS3h inhibition by QU663. The resulting three-dimensional interaction model is discussed... - 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 activityCaterina Fattorusso
Dipartimento di Chimica delle Sostanze Naturali, Universita' di Napoli Federico II, Via D. Montesano 49, 80131 Napoli, Italy
J Med Chem 48:7153-65. 2005..Among the pyrrolobenzoxazepines investigated, 15c appeared to be the most promising NNRTI of the series characterized by potent antiviral activity, broad spectrum, and low cytotoxicity. 15c showed synergistic antiviral activity with AZT... - Endoperoxide derivatives from marine organisms: 1,2-dioxanes of the plakortin family as novel antimalarial agentsCaterina Fattorusso
Dipartimento di Chimica delle Sostanze Naturali, Universita di Napoli Federico II, via D Montesano 49, 80131 Napoli, Italy
J Med Chem 49:7088-94. 2006.... - Conformational flexibility in the peripheral site of Torpedo californica acetylcholinesterase revealed by the complex structure with a bifunctional inhibitorJacques Ph Colletier
, Institut de Biologie Structurale, 38027 Grenoble, France
J Am Chem Soc 128:4526-7. 2006..The observed conformational flexibility highlights the dynamic nature of protein structures and is of importance for structure-based drug design... - 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 vivoLisa M Greene
Department of Biochemistry, Trinity College, Dublin 2, Ireland
Oncol Rep 14:1357-63. 2005..5 mg/kg) significantly inhibited tumour growth in vivo in a mouse mammary carcinoma model (p=0.04, n=5, Student's t-test). Thus, PBOX-6 could be a promising anti-cancer agent for both hormone-dependent and -independent breast cancers... - ST2472: a new potential antipsychotic with very low liability to induce side-effectsMaria A Stasi
Sigma Tau Industrie Farmaceutiche Riunite S p A, Pomezia, Rome, Italy
Int J Neuropsychopharmacol 11:309-19. 2008..In conclusion, ST2472 seems to be an antipsychotic with lower liability to produce side-effects than other antipsychotics, such as haloperidol, risperidone, olanzapine and clozapine, which were evaluated as reference drugs... - Selective targeting of the HIV-1 reverse transcriptase catalytic complex through interaction with the "primer grip" region by pyrrolobenzoxazepinone non-nucleoside inhibitors correlates with increased activity towards drug-resistant mutantsSamantha Zanoli
Institute of Molecular Genetics, IGM CNR, via Abbiategrasso 207, I 27100 Pavia, Italy
Biochem Pharmacol 76:156-68. 2008..Molecular modeling and docking studies provided an explanation for this correlation at the structural level... - BubR1 is required for a sustained mitotic spindle checkpoint arrest in human cancer cells treated with tubulin-targeting pyrrolo-1,5-benzoxazepinesLisa M Greene
School of Biochemistry and Immunology, Trinity College, Dublin 2, United Kingdom
Mol Pharmacol 73:419-30. 2008..Taken together, these results suggest that BubR1 contributes to the mitotic checkpoint induced by the PBOXs... - Selective induction of apoptosis by the pyrrolo-1,5-benzoxazepine 7-[[dimethylcarbamoyl]oxy]-6-(2-naphthyl)pyrrolo-[2,1-d] (1,5)-benzoxazepine (PBOX-6) in Leukemia cells occurs via the c-Jun NH2-terminal kinase-dependent phosphorylation and inactivation oMargaret M Mc Gee
Department of Biochemistry, Trinity College, Dublin 2, Ireland
J Pharmacol Exp Ther 310:1084-95. 2004..Collectively, these findings identify Bcl-2 phosphorylation and inactivation as a critical step in the apoptotic pathway induced by PBOX-6 and highlight its potential as an effective antileukemic agent... - Caspase-3 is not essential for DNA fragmentation in MCF-7 cells during apoptosis induced by the pyrrolo-1,5-benzoxazepine, PBOX-6Margaret M Mc Gee
Biochemistry Department, Trinity College, 2, Dublin, Ireland
FEBS Lett 515:66-70. 2002..This study suggests that caspase-3 is not necessarily essential for DNA fragmentation and the morphological changes associated with apoptosis... - Benzoxepin-derived estrogen receptor modulators: a novel molecular scaffold for the estrogen receptorDavid G Lloyd
Department of Biochemistry, Trinity College Dublin, Dublin 2, Ireland
J Med Chem 47:5612-5. 2004..The effect of functional group substitution on the benzoxepin scaffold is explored through a brief computational structure-activity relationship investigation with molecular simulation... - Activation of the c-Jun N-terminal kinase (JNK) signaling pathway is essential during PBOX-6-induced apoptosis in chronic myelogenous leukemia (CML) cellsMargaret M Mc Gee
Department of Biochemistry, Trinity College, Dublin 2, Ireland
J Biol Chem 277:18383-9. 2002..JIP-1 specifically scaffolds JNK, MKK7, and members of the mixed-lineage kinase (MLK) family, implicating these kinases upstream of JNK in the apoptotic pathway induced by PBOX-6 in K562 cells... - A new microtubule-targeting compound PBOX-15 inhibits T-cell migration via post-translational modifications of tubulinNavin K Verma
Department of Clinical Medicine, Institute of Molecular Medicine, Trinity College Dublin, Dublin, Ireland
J Mol Med (Berl) 86:457-69. 2008..Novel microtubule-targeting effects of PBOX-15 can possibly open new horizons in the treatment of overactive inflammatory conditions as well as cancer and cancer metastatic spreading...