Lucia Altucci

Summary

Affiliation: University of Rome La Sapienza
Country: Italy

Publications

  1. ncbi request reprint Synthesis and biological validation of novel synthetic histone/protein methyltransferase inhibitors
    Antonello Mai
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Universita degli Studi di Roma La Sapienza, P le A Moro 5, 00185 Roma, Italy
    ChemMedChem 2:987-91. 2007
  2. ncbi request reprint 3-(4-Aroyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-alkylamides as a new class of synthetic histone deacetylase inhibitors. 1. Design, synthesis, biological evaluation, and binding mode studies performed through three different docking procedures
    Antonello Mai
    Dipartimento di Studi Farmaceutici, Universita degli Studi di Roma La Sapienza, P le A Moro 5, 00185 Roma, Italy
    J Med Chem 46:512-24. 2003
  3. ncbi request reprint Small molecule inhibitors of histone arginine methyltransferases: homology modeling, molecular docking, binding mode analysis, and biological evaluations
    Rino Ragno
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Universita degli Studi di Roma La Sapienza, P le Aldo Moro 5, I 00185 Roma
    J Med Chem 50:1241-53. 2007
  4. ncbi request reprint Novel pyrrole-containing histone deacetylase inhibitors endowed with cytodifferentiation activity
    Antonello Mai
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Universita degli Studi di Roma La Sapienza, Piazzale A Moro 5, 00185 Rome, Italy
    Int J Biochem Cell Biol 39:1510-22. 2007
  5. doi request reprint HDAC-class II specific inhibition involves HDAC proteasome-dependent degradation mediated by RANBP2
    Annamaria Scognamiglio
    Dipartimento di Patologia Generale, Seconda Universita degli Studi di Napoli, Vico L De Crecchio 7, 80138 Napoli, Italy
    Biochim Biophys Acta 1783:2030-8. 2008
  6. pmc Identification of specific and semi-specific SIRT inhibitors through computer-aided studies
    Antonello Mai
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Universita di Roma, Roma, Italy
    Aging (Albany NY) 3:819-20. 2011
  7. doi request reprint Small-molecule inhibitors of histone deacetylase for the treatment of cancer and non-cancer diseases: a patent review (2011 - 2013)
    Sergio Valente
    Sapienza Universita di Roma, Dipartimento di Chimica e Tecnologie del Farmaco, P le A Moro 5, 00185 Roma, Italy 39 064 991 3392 39 064 969 3268
    Expert Opin Ther Pat 24:401-15. 2014
  8. pmc The emerging role of histone lysine demethylases in prostate cancer
    Francesco Crea
    Experimental Therapeutics, British Columbia Cancer Research Centre, 675 West 10th Avenue, Vancouver, BC, Canada, V5Z 1L3
    Mol Cancer 11:52. 2012
  9. ncbi request reprint Small-molecule inhibitors of histone acetyltransferase activity: identification and biological properties
    Antonello Mai
    Dipartimento di Studi Farmaceutici, Istituto Pasteur Fondazione Cenci Bolognetti, Universita degli Studi di Roma La Sapienza, P le A Moro 5, 00185 Roma, Italy
    J Med Chem 49:6897-907. 2006
  10. doi request reprint Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities
    Antonello Mai
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Sapienza Universita di Roma, P le A Moro 5, 00185 Roma, Italy
    Bioorg Med Chem Lett 18:2530-5. 2008

Collaborators

Detail Information

Publications76

  1. ncbi request reprint Synthesis and biological validation of novel synthetic histone/protein methyltransferase inhibitors
    Antonello Mai
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Universita degli Studi di Roma La Sapienza, P le A Moro 5, 00185 Roma, Italy
    ChemMedChem 2:987-91. 2007
  2. ncbi request reprint 3-(4-Aroyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-alkylamides as a new class of synthetic histone deacetylase inhibitors. 1. Design, synthesis, biological evaluation, and binding mode studies performed through three different docking procedures
    Antonello Mai
    Dipartimento di Studi Farmaceutici, Universita degli Studi di Roma La Sapienza, P le A Moro 5, 00185 Roma, Italy
    J Med Chem 46:512-24. 2003
    ..The enhanced fit allows a closer positioning of 8 hydroxamate moiety to the zinc ion. These findings were supported by extensive docking studies (SAD, DOCK, and Autodock) performed on both APHAs and reference drugs (TSA and SAHA)...
  3. ncbi request reprint Small molecule inhibitors of histone arginine methyltransferases: homology modeling, molecular docking, binding mode analysis, and biological evaluations
    Rino Ragno
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Universita degli Studi di Roma La Sapienza, P le Aldo Moro 5, I 00185 Roma
    J Med Chem 50:1241-53. 2007
    ..These regions should be taken into account in the design of novel PRMT inhibitors...
  4. ncbi request reprint Novel pyrrole-containing histone deacetylase inhibitors endowed with cytodifferentiation activity
    Antonello Mai
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Universita degli Studi di Roma La Sapienza, Piazzale A Moro 5, 00185 Rome, Italy
    Int J Biochem Cell Biol 39:1510-22. 2007
    ..Tested to evaluate their effects on histone H3 and alpha-tubulin acetylation, 3b and 4a showed high H3 acetylation, whereas 4a and 4b were the most potent with alpha-tubulin as a substrate...
  5. doi request reprint HDAC-class II specific inhibition involves HDAC proteasome-dependent degradation mediated by RANBP2
    Annamaria Scognamiglio
    Dipartimento di Patologia Generale, Seconda Universita degli Studi di Napoli, Vico L De Crecchio 7, 80138 Napoli, Italy
    Biochim Biophys Acta 1783:2030-8. 2008
    ..These findings identify a crosstalk occurring between acetylation, deacetylation and sumoylation pathways and suggest that class II specific HDAC inhibitors may affect different epigenetic pathways...
  6. pmc Identification of specific and semi-specific SIRT inhibitors through computer-aided studies
    Antonello Mai
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Universita di Roma, Roma, Italy
    Aging (Albany NY) 3:819-20. 2011
    ..Comment on: Schlicker C et al. Structure-based Development of Novel Sirtuin Inhibitors. Aging. 2011; 3:issue 9...
  7. doi request reprint Small-molecule inhibitors of histone deacetylase for the treatment of cancer and non-cancer diseases: a patent review (2011 - 2013)
    Sergio Valente
    Sapienza Universita di Roma, Dipartimento di Chimica e Tecnologie del Farmaco, P le A Moro 5, 00185 Roma, Italy 39 064 991 3392 39 064 969 3268
    Expert Opin Ther Pat 24:401-15. 2014
    ..Different chemical entities have been developed in the recent years and some of them entered clinical trials...
  8. pmc The emerging role of histone lysine demethylases in prostate cancer
    Francesco Crea
    Experimental Therapeutics, British Columbia Cancer Research Centre, 675 West 10th Avenue, Vancouver, BC, Canada, V5Z 1L3
    Mol Cancer 11:52. 2012
    ..Finally, we explore the role of KDMs as novel prognostic factors and therapeutic targets. We believe that studies on histone demethylation may add a novel perspective in our efforts to prevent and cure advanced PCa...
  9. ncbi request reprint Small-molecule inhibitors of histone acetyltransferase activity: identification and biological properties
    Antonello Mai
    Dipartimento di Studi Farmaceutici, Istituto Pasteur Fondazione Cenci Bolognetti, Universita degli Studi di Roma La Sapienza, P le A Moro 5, 00185 Roma, Italy
    J Med Chem 49:6897-907. 2006
    ..In the same assay, 22 at lower concentration (100 microM) showed the same hypoacetylating effects with both histone and non-histone substrates...
  10. doi request reprint Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities
    Antonello Mai
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Sapienza Universita di Roma, P le A Moro 5, 00185 Roma, Italy
    Bioorg Med Chem Lett 18:2530-5. 2008
    ..Surprisingly, the highest differentiation was observed with 13, through an effect that seems to be unrelated to HDAC inhibition...
  11. ncbi request reprint Aroyl-pyrrolyl hydroxyamides: influence of pyrrole C4-phenylacetyl substitution on histone deacetylase inhibition
    Antonello Mai
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Universita degli Studi di Roma La Sapienza, P le A Moro 5, 00185 Roma, Italy
    ChemMedChem 1:225-37. 2006
    ..Compound 4 b showed interesting, dose-dependent antiproliferative and cytodifferentiation properties against human acute promyelocytic leukemia HL-60 cells...
  12. doi request reprint Epi-drugs to fight cancer: from chemistry to cancer treatment, the road ahead
    Antonello Mai
    Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Universita di Roma, 00185 Roma, IT, Italy
    Int J Biochem Cell Biol 41:199-213. 2009
    ..In this review we will focus on the chemical aspects of such molecules, joined to their effective (or potential) application in cancer therapy...
  13. ncbi request reprint Synthesis and biological evaluation of 2-, 3-, and 4-acylaminocinnamyl-N-hydroxyamides as novel synthetic HDAC inhibitors
    A Mai
    Dipartimento di Studi Farmaceutici, Istituto Pasteur, Fondazione Cenci Bolognetti, Universita degli Studi di Roma La Sapienza, P le A Moro 5, 00185 Roma, Italy
    Med Chem 1:245-54. 2005
    ..Selected 2 and 3 compounds will be evaluated to determine their antiproliferative and cyto differentiating activities on HL-60 cells...
  14. ncbi request reprint Synthesis and biological properties of novel, uracil-containing histone deacetylase inhibitors
    Antonello Mai
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Universita degli Studi di Roma La Sapienza, P le A Moro 5, 00185 Roma, Italy
    J Med Chem 49:6046-56. 2006
    ..The tested UBHAs displayed weak p21WAF1/CIP1 induction in U937 cells, and 1d and 1j showed high histone H3 and alpha-tubulin acetylation effects...
  15. ncbi request reprint Design, synthesis, and biological evaluation of sirtinol analogues as class III histone/protein deacetylase (Sirtuin) inhibitors
    Antonello Mai
    Dipartimento di Studi Farmaceutici, Istituto Pasteur, Fondazione Cenci Bolognetti, Universita degli Studi di Roma La Sapienza, P le A Moro 5, 00185 Roma, Italy
    J Med Chem 48:7789-95. 2005
    ..3-13 times less potent than sirtinol, whereas the 2'-carboxamido analogue was totally inactive. Both (R)- and (S)-sirtinol had similar inhibitory effects on the yeast and human enzymes, demonstrating no enantioselective inhibitory effect...
  16. ncbi request reprint Discovery of uracil-based histone deacetylase inhibitors able to reduce acquired antifungal resistance and trailing growth in Candida albicans
    Antonello Mai
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Universita degli Studi di Roma La Sapienza, P le A Moro 5, 00185 Roma, Italy
    Bioorg Med Chem Lett 17:1221-5. 2007
    ..In this assay, 1c,d were more potent than SAHA, a well-known HDAC inhibitor, in reducing the Candida growth. More interestingly, 1c,d as well as SAHA were able to inhibit the fluconazole-induced resistance induction in Candida cultures...
  17. ncbi request reprint Histone deacetylase inhibitors and neurodegenerative disorders: holding the promise
    Antonello Mai
    Pasteur Institute, Cenci Bolognetti Foundation, Department of Drug Chemistry and Technologies, University of Rome La Sapienza, P le A Moro 5, 00185 Rome, Italy
    Curr Pharm Des 15:3940-57. 2009
    ..Here we survey most of the recent applications of HDAC inhibitors in the cited NDs, and we make the point of our (up to now) knowledge about the involvement of singular HDAC/SIRT isoform in NDs and other CNS pathologies...
  18. doi request reprint New pyrrole-based histone deacetylase inhibitors: binding mode, enzyme- and cell-based investigations
    Antonello Mai
    Dipartimento di Studi Farmaceutici, Sapienza Universita di Roma, 00185 Roma, Italy
    Int J Biochem Cell Biol 41:235-47. 2009
    ..When tested in the human leukaemia U937 cell line, 4i showed altered cell cycle (S phase arrest), joined to high (51%) apoptosis induction and significant (21%) differentiation activity...
  19. doi request reprint epigenetic multiple ligands: mixed histone/protein methyltransferase, acetyltransferase, and class III deacetylase (sirtuin) inhibitors
    Antonello Mai
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Universita degli Studi di Roma La Sapienza, Piazzale A Moro 5, 00185 Rome, Italy
    J Med Chem 51:2279-90. 2008
    ..e., 40.7% ( 4l) and 42.6% ( 7b)] and/or massive, dose-dependent cytodifferentiation [i.e., 95.2% ( 1c) and 96.1% ( 4j)], whereas the single-target inhibitors eosin, curcumin, and sirtinol were ineffective or showed a weak effect...
  20. doi request reprint Identification of 4-hydroxyquinolines inhibitors of p300/CBP histone acetyltransferases
    Antonello Mai
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Universita di Roma, P le A Moro 5, 00185 Roma, Italy
    Bioorg Med Chem Lett 19:1132-5. 2009
    ..When tested in U937 cells, some compounds displayed pro-apoptotic or cytodifferentiating properties...
  21. ncbi request reprint Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains
    Antonello Mai
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Universita degli Studi di Roma La Sapienza, P le A Moro 5, 00185 Roma, Italy
    J Med Chem 50:5412-24. 2007
    ..The higher inhibitor adaptability to the HIV-1 RT non-nucleoside binding site (NNBS) may account for the higher inhibitory effect exerted by the new molecules against the mutated RTs...
  22. ncbi request reprint The therapeutic uses of chromatin-modifying agents
    Antonello Mai
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Universita di Roma La Sapienza, Piazzale Aldo Moro 5, I 00185 Roma, Italy
    Expert Opin Ther Targets 11:835-51. 2007
    ..Only a few HMTi have been described to date, but these small molecules could be a useful scaffold to discovering new highly active and enzyme-selective compounds to develop as therapeutics...
  23. doi request reprint Study of 1,4-dihydropyridine structural scaffold: discovery of novel sirtuin activators and inhibitors
    Antonello Mai
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, Universita degli Studi di Roma La Sapienza, Roma, Italy
    J Med Chem 52:5496-504. 2009
    ..Senescence assays performed on hMSC and mitochondrial function studies conducted with murine C2C12 myoblasts confirmed the compounds' novel and unique SIRT-activating properties...
  24. doi request reprint Small-molecule chromatin-modifying agents: therapeutic applications
    Antonello Mai
    Pasteur Institute Cenci Bolognetti Foundation, Drug Chemistry and Technologies Department, University of Rome Sapienza, Piazzale Aldo Moro 5, Rome, Italy
    Epigenomics 2:307-24. 2010
    ..Furthermore, the SIRT2-selective AGK-2 has been reported to have protective effects against Parkinson's disease, and resveratrol and other sirtuin activators can be useful for the treatment of Alzheimer's disease...
  25. ncbi request reprint Exploring the connection unit in the HDAC inhibitor pharmacophore model: novel uracil-based hydroxamates
    Antonello Mai
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Universita degli Studi di Roma La Sapienza, P le A Moro 5, 00185 Roma, Italy
    Bioorg Med Chem Lett 15:4656-61. 2005
    ..Such compounds also caused hyperacetylation in NIH3T3 cell core histones and were endowed with interesting antiproliferative and cytodifferentiating effects in human leukemia (HL-60) cells...
  26. ncbi request reprint 3-(4-Aroyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamides as a new class of synthetic histone deacetylase inhibitors. 2. Effect of pyrrole-C2 and/or -C4 substitutions on biological activity
    Antonello Mai
    Dipartimento di Studi Farmaceutici, Universita degli Studi di Roma La Sapienza, P le A Moro 5, 00185 Roma, Italy
    J Med Chem 47:1098-109. 2004
    ....
  27. ncbi request reprint Discovery of (aryloxopropenyl)pyrrolyl hydroxyamides as selective inhibitors of class IIa histone deacetylase homologue HD1-A
    Antonello Mai
    Dipartimento di Studi Farmaceutici, Universita degli Studi di Roma La Sapienza, P le A Moro 5, 00185 Roma, Italy
    J Med Chem 46:4826-9. 2003
    ..They could be useful as tools for probing the biology of these enzymes and eventually as new anticancer agents with low toxicity...
  28. ncbi request reprint Binding mode analysis of 3-(4-benzoyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamide: a new synthetic histone deacetylase inhibitor inducing histone hyperacetylation, growth inhibition, and terminal cell differentiation
    Antonello Mai
    Dipartimento di Studi Farmaceutici, Universita degli Studi di Roma La Sapienza, P le A Moro 5, 00185 Roma, Italy
    J Med Chem 45:1778-84. 2002
    ....
  29. ncbi request reprint Synthesis and biological evaluation of enantiomerically pure pyrrolyl-oxazolidinones as a new class of potent and selective monoamine oxidase type A inhibitors
    A Mai
    Dipartimento Studi Farmaceutici, Universita degli Studi di Roma La Sapienza, Ple A Moro 5, 00185 Rome, Italy
    Farmaco 58:231-41. 2003
    ..The most potent compound is (R)-5-methoxymethyl-3-(1H-pyrrol-1-yl)-2-oxazolidinone (1b), endowed with very high potency (K(iMAO-A) = 4.9 nM) and A-selectivity (A-selectivity = 10,200, about 116-fold greater than that of befloxatone)...
  30. ncbi request reprint 3-(4-Aroyl-1-methyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides as a new class of synthetic histone deacetylase inhibitors. 3. Discovery of novel lead compounds through structure-based drug design and docking studies
    Rino Ragno
    Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Universita degli Studi di Roma La Sapienza, P le A Moro 5, 00185 Roma, Italy
    J Med Chem 47:1351-9. 2004
    ..Compound 4, tested as antiproliferative and cytodifferentiating agent on MEL cells, showed dose-dependent growth inhibition and hemoglobin accumulation effects...
  31. ncbi request reprint Class II (IIa)-selective histone deacetylase inhibitors. 1. Synthesis and biological evaluation of novel (aryloxopropenyl)pyrrolyl hydroxyamides
    Antonello Mai
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Universita degli Studi di Roma La Sapienza, P le A Moro 5, 00185 Roma, Italy
    J Med Chem 48:3344-53. 2005
    ....
  32. ncbi request reprint Histone deacetylation in epigenetics: an attractive target for anticancer therapy
    Antonello Mai
    Istituto Pasteur, Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Universita degli Studi di Roma La Sapienza, P le A Moro 5, 00185 Roma, Italy
    Med Res Rev 25:261-309. 2005
    ....
  33. doi request reprint Novel cinnamyl hydroxyamides and 2-aminoanilides as histone deacetylase inhibitors: apoptotic induction and cytodifferentiation activity
    Sergio Valente
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, Universita degli Studi di Roma La Sapienza, P le A Moro 5, 00185 Roma, Italy
    ChemMedChem 6:698-712. 2011
    ..The highest-scoring derivatives in terms of apoptosis (1 k, 1 l) or cytodifferentiation (2 c, 4 n) also showed antiproliferative activity in U937 cells, thus representing valuable tools for study in other cancer contexts...
  34. pmc Molecular analysis of the effects of Piroxicam and Cisplatin on mesothelioma cells growth and viability
    Alessandra Verdina
    Laboratory D, Dept for Development of Therapeutic Programs, CRS, Regina Elena Cancer Institute, Via delle Messi d Oro 156, 00158, Rome, Italy
    J Transl Med 6:27. 2008
    ..These results suggest that the association of piroxicam and CDDP specifically triggers cell cycle regulation and apoptosis in different mesothelioma cell lines and may hold promise in the treatment of mesothelioma...
  35. doi request reprint Discovery of salermide-related sirtuin inhibitors: binding mode studies and antiproliferative effects in cancer cells including cancer stem cells
    Dante Rotili
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, Universita degli Studi di Roma La Sapienza, P le A Moro 5, 00185 Roma, Italy
    J Med Chem 55:10937-47. 2012
    ..Such compounds will be further explored for their broad-spectrum anticancer properties...
  36. doi request reprint tert-Butylcarbamate-containing histone deacetylase inhibitors: apoptosis induction, cytodifferentiation, and antiproliferative activities in cancer cells
    Sergio Valente
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Universita di Roma, P le A Moro 5, 00185 Roma, Italy
    ChemMedChem 8:800-11. 2013
    ..In HT29 cells, 10 c increased histone H3 acetylation, and decreased the colony-forming potential of the cancer cells by up to 60 %...
  37. doi request reprint Identification of PR-SET7 and EZH2 selective inhibitors inducing cell death in human leukemia U937 cells
    Sergio Valente
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Universita di Roma, P le A Moro 5, 00185 Roma, Italy
    Biochimie 94:2308-13. 2012
    ..9 μM), tested in U937 cells at 50 μM, induced massive cell death and 28% of granulocytic differentiation, highlighting the potential use of EZH2 inhibitors in cancer...
  38. ncbi request reprint Identification of two new synthetic histone deacetylase inhibitors that modulate globin gene expression in erythroid cells from healthy donors and patients with thalassemia
    Antonello Mai
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Universita degli Studi di Roma La Sapienza, Roma, Italy
    Mol Pharmacol 72:1111-23. 2007
    ..The low toxicity exerted by compounds 9 and 24 in all of the assays investigated suggests that these new HDAC inhibitors should be considered for personalized therapy of selected patients with beta(0) thalassemia...
  39. doi request reprint Simplification of the tetracyclic SIRT1-selective inhibitor MC2141: coumarin- and pyrimidine-based SIRT1/2 inhibitors with different selectivity profile
    Dante Rotili
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, Universita degli Studi di Roma La Sapienza, P le A Moro 5, 00185 Roma, Italy
    Bioorg Med Chem 19:3659-68. 2011
    ..Such compounds, differently from the unselective prototype, are endowed with a selective inhibition of SIRT1 over SIRT2, and, in some cases (6j, 6k, and 6q), are more efficient than 3 to induce apoptosis in U937 cells...
  40. ncbi request reprint Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptase
    A Mai
    Istituto Pasteur-Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, , P.le A. Moro 5, I-00185 Roma, Italy
    J Med Chem 44:2544-54. 2001
    ....
  41. ncbi request reprint Structure-activity relationship studies on new DABOS: effect of substitutions at pyrimidine C-5 and C-6 positions on anti-HIV-1 activity
    G Sbardella
    Farmaceutici Istituto Pasteur-Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, , La Sapienza, Italy
    Antivir Chem Chemother 12:37-50. 2001
    ..2-Alkylthio-3,4-dihydropyrimidin-4(3H)-one derivatives of F2-S-DABO series bearing small alkyl groups at C-5 proved to be potent inhibitors of HIV-1 replication in vitro with selectivity indexes ranging from 250 to >2,500...
  42. ncbi request reprint Carprofen analogues as sirtuin inhibitors: enzyme and cellular studies
    Paolo Mellini
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Universita di Roma, P le A Moro 5, 00185 Roma Italy
    ChemMedChem 7:1905-8. 2012
    ..The most potent compound (shown) increased acetyl-p53 and acetyl-α-tubulin levels, and induced slight apoptosis at 50 μM in U937 cells, differently from selisistat and carprofen. ..
  43. ncbi request reprint Chiral resolution and molecular modeling investigation of rac-2-cyclopentylthio-6-[1-(2,6-difluorophenyl)ethyl]-3,4-dihydro-5-methylpyrimidin-4(3H)-one (MC-1047), a potent anti-HIV-1 reverse transcriptase agent of the DABO class
    M Quaglia
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Universita degli Studi di Roma La Sapienza, Roma, Italy
    Chirality 13:75-80. 2001
    ....
  44. doi request reprint Pan-histone demethylase inhibitors simultaneously targeting Jumonji C and lysine-specific demethylases display high anticancer activities
    Dante Rotili
    Department of Drug Chemistry and Technologies, Sapienza University of Rome, P le A Moro 5, 00185 Rome, Italy
    J Med Chem 57:42-55. 2014
    ..When tested in noncancer mesenchymal progenitor (MePR) cells, 2 and 3 induced little and no apoptosis, respectively, thus showing cancer-selective inhibiting action. ..
  45. ncbi request reprint Benzodeazaoxaflavins as sirtuin inhibitors with antiproliferative properties in cancer stem cells
    Dante Rotili
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Universita di Roma, Piazzale Aldo Moro 5, 00185 Roma, Italy
    J Med Chem 55:8193-7. 2012
    ....
  46. pmc "Shock and kill" effects of class I-selective histone deacetylase inhibitors in combination with the glutathione synthesis inhibitor buthionine sulfoximine in cell line models for HIV-1 quiescence
    Andrea Savarino
    Dept of Infectious, Parasitic and Immune Mediated Diseases, Istituto Superiore di Sanita, Viale Regina Elena, 299, 00161, Rome, Italy
    Retrovirology 6:52. 2009
    ....
  47. ncbi request reprint 3-(1H-pyrrol-2-yl)-2-oxazolidinones as novel monoamine oxidase type A inhibitors
    A Mai
    Dipartimento di Studi Farmaceutici, Universita degli Studi di Roma La Sapienza, P le A Moro 5, 00185 Roma, Italy
    Med Chem 1:117-24. 2005
    ..Such results indicate that 2a-s may represent a new promising series of antidepressant agents...
  48. ncbi request reprint 5-Alkyl-2-alkylamino-6-(2,6-difluorophenylalkyl)-3,4-dihydropyrimidin-4(3H)-ones, a new series of potent, broad-spectrum non-nucleoside reverse transcriptase inhibitors belonging to the DABO family
    Antonello Mai
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Universita degli Studi di Roma La Sapienza, P le A Moro 5, I 00185 Roma, Italy
    Bioorg Med Chem 13:2065-77. 2005
    ....
  49. ncbi request reprint Nitroquinolones with broad-spectrum antimycobacterial activity in vitro
    M Artico
    Dipartimento di Studi Farmaceutici, Universita di Roma La Sapienza, Italy
    Bioorg Med Chem Lett 9:1651-6. 1999
    ..Some 6-nitroquinolones were found to exert good inhibiting activities against Mycobacterium tuberculosis and various atypical mycobacteria, whereas the 6-fluoro counterparts showed poor or no activity against this bacterium...
  50. ncbi request reprint A novel Gcn5p inhibitor represses cell growth, gene transcription and histone acetylation in budding yeast
    Prisca Ornaghi
    Dipartimento Genetica e Biologia Molecolare, Universita degli Studi di Roma La Sapienza, P le A Moro 5, I 00185 Roma, Italy
    Biochem Pharmacol 70:911-7. 2005
    ..In addition, our results demonstrate that MC1626 is a Gcn5p-dependent yeast growth inhibitor...
  51. doi request reprint Combining 3-D quantitative structure-activity relationship with ligand based and structure based alignment procedures for in silico screening of new hepatitis C virus NS5B polymerase inhibitors
    Ira Musmuca
    Dipartimento di Chimica e Tecnologie del Farmaco, Istituto Pasteur Fondazione Cenci Bolognetti, Sapienza Universita di Roma, P le A Moro 5, 00185 Rome, Italy
    J Chem Inf Model 50:662-76. 2010
    ..Binding mode analysis of hit compounds within the NS5B polymerase thumb domain showed that one of them, NSC 123526, exhibited a docked conformation which was in good agreement with the thumb training set most active compound (6)...
  52. ncbi request reprint Evaluation of a large library of (thiazol-2-yl)hydrazones and analogues as histone acetyltransferase inhibitors: Enzyme and cellular studies
    Simone Carradori
    Department of Drug Chemistry and Technologies, Sapienza University of Rome, P le A Moro 5, 00185 Rome, Italy
    Eur J Med Chem 80:569-78. 2014
    ....
  53. doi request reprint Laccase treatment impairs bisphenol A-induced cancer cell proliferation affecting estrogen receptor alpha-dependent rapid signals
    Alessandro Bolli
    Department of Biology, University Roma Tre, Viale Guglielmo Marconi 446, Roma, Italy
    IUBMB Life 60:843-52. 2008
    ..Moreover, the laccase-catalyzed oxidation of BPA reduces the BPA cytotoxic effect. Thus, laccase appears to impair BPA action(s), representing an invaluable bioremediation enzyme...
  54. ncbi request reprint N-[4-(1,1'-biphenyl)methyl]-4-(4-thiomorpholinylmethyl) benzenamines as non-oxazolidinone analogues of antimycobacterial U-100480
    M Artico
    Dipartimento di Studi Farmaceutici, Universita di Roma La Sapienza, Italy
    Bioorg Med Chem Lett 8:1493-8. 1998
    ..Some biphenyl derivatives were endowed with high activity against Mycobacterium tuberculosis and other non-tuberculous mycobacteria...
  55. ncbi request reprint Class II-selective histone deacetylase inhibitors. Part 2: alignment-independent GRIND 3-D QSAR, homology and docking studies
    Rino Ragno
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Universita degli Studi di Roma La Sapienza, P le A Moro 5, 00185 Roma, Italy
    Eur J Med Chem 43:621-32. 2008
    ..The same conclusions could be achieved by molecular docking studies of the most selective inhibitors...
  56. ncbi request reprint Computer-aided design, synthesis, and anti-HIV-1 activity in vitro of 2-alkylamino-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as novel potent non-nucleoside reverse transcriptase inhibitors, also active against the Y181C varia
    Rino Ragno
    Dipartimento di Studi di Chimica e Tecnologie delle Sostanze Biologicamente Attive, Universita degli Studi di Roma La Sapienza, P le A Moro 5, I 00185 Roma, Italy
    J Med Chem 47:928-34. 2004
    ....
  57. ncbi request reprint 3-D QSAR studies on histone deacetylase inhibitors. A GOLPE/GRID approach on different series of compounds
    Rino Ragno
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Universita degli Studi di Roma La Sapienza, P le A Moro 5, 00185 Roma, Italy
    J Chem Inf Model 46:1420-30. 2006
    ..To our knowledge this is the first 3-D QSAR application on a broad molecular diversity training set of HDACIs...
  58. ncbi request reprint Piroxicam and cisplatin in a mouse model of peritoneal mesothelioma
    Enrico P Spugnini
    SAFU Department, CRS, Regina Elena Cancer Institute, Rome, Italy
    Clin Cancer Res 12:6133-43. 2006
    ..The aim of the present study was to evaluate the effects of piroxicam, a widely used nonsteroidal anti-inflammatory drug, alone and in combination with cisplatin (CDDP), on cell growth of mesothelioma cells...
  59. ncbi request reprint Non-cancer uses of histone deacetylase inhibitors: effects on infectious diseases and beta-hemoglobinopathies
    Dante Rotili
    Pasteur Institute, Cenci Bolognetti Foundation, Department of Drug Chemistry and Technologies, Sapienza University of Rome, p le A Moro, 5, 00185, Rome, Italy
    Curr Top Med Chem 9:272-91. 2009
    ....
  60. ncbi request reprint Analytical and semipreparative high performance liquid chromatography separation of stereoisomers of novel 3,4-dihydropyrimidin-4(3H)-one derivatives on the immobilised amylose-based Chiralpak IA chiral stationary phase
    Roberto Cirilli
    Dipartimento del Farmaco, Istituto Superiore di Sanita, Roma, Italy
    J Sep Sci 29:1399-406. 2006
    ..In order to study the chiroptical properties of single stereoisomers, mg-scale separations were performed on analytical and semipreparative size Chiralpak IA columns in combination with ethyl acetate-based eluents...
  61. doi request reprint Epigenetic modulation of PGC-1α activity by GCN5 inhibitors: WO2010007085
    Simone Carradori
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza University of Rome, P A Moro 5, 00185 Rome, Italy
    Expert Opin Ther Pat 21:1651-6. 2011
    ..Thus, both GCN5 and SIRT1 may be pharmacological targets to regulate the activity of PGC-1α, providing a potential treatment for metabolic disorders in which hepatic glucose output is altered...
  62. ncbi request reprint 3-(1H-Pyrrol-1-yl)-2-oxazolidinones as reversible, highly potent, and selective inhibitors of monoamine oxidase type A
    Antonello Mai
    Dipartimento di Studi Farmaceutici, Universita degli Studi di Roma La Sapienza, P le A Moro 5, 00185 Roma, Italy
    J Med Chem 45:1180-3. 2002
    ..R)-5-Methoxymethyl-3-(1H-pyrrol-1-yl)-2-oxazolidinone 1b, the most potent among test derivatives, was 78-fold more potent than toloxatone...
  63. ncbi request reprint 6-[1-(2,6-difluorophenyl)ethyl]pyrimidinones antagonize cell proliferation and induce cell differentiation by inhibiting (a nontelomeric) endogenous reverse transcriptase
    Sara Bartolini
    Istituto Superiore di Sanita, Viale Regina Elena 299, Via del Castro Laurenziano 25, 00161 Rome, Italy
    J Med Chem 48:6776-8. 2005
    ..These results propose F(2)-DABOs as useful tools in preventive and/or curative therapy to counteract the loss of differentiation in dedifferentiating pathologies and as antiproliferative drugs in tumor therapy...
  64. ncbi request reprint New 6-nitroquinolones: synthesis and antimicrobial activities
    Gianluca Sbardella
    Dipartimento di Scienze Farmaceutiche, Universita degli Studi di Salerno, Via Ponte Don Melillo, 84084 Fisciano SA, Italy
    Farmaco 59:463-71. 2004
    ..Some derivatives were also found more potent than ciprofloxacin and ofloxacin (used as reference drugs) against gram-positive bacteria...
  65. pmc Antimalarial and antileishmanial activities of aroyl-pyrrolyl-hydroxyamides, a new class of histone deacetylase inhibitors
    Antonello Mai
    Antimicrob Agents Chemother 48:1435-6. 2004
  66. ncbi request reprint Inhibition of histone deacetylase class I but not class II is critical for the sensitization of leukemic cells to tumor necrosis factor-related apoptosis-inducing ligand-induced apoptosis
    Satoshi Inoue
    Medical Research Council Toxicology Unit, University of Leicester, Lancaster Road, Leicester LE1 9HN, United Kingdom
    Cancer Res 66:6785-92. 2006
    ....
  67. ncbi request reprint 6-alkylthio-4-[1-(2,6-difluorophenyl)alkyl]-1H-[1,3,5]triazin-2-ones (ADATs): novel regulators of cell differentiation and proliferation
    Gianluca Sbardella
    Dipartimento di Scienze Farmaceutiche Università degli Studi di Salerno Via Ponte Don Melillo, Fisciano SA, Italy
    ChemMedChem 1:1073-80. 2006
    ..These results support the potential of NNRTIs as valuable antitumor agents...
  68. doi request reprint 5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile
    Maxim B Nawrozkij
    Volgograd State Technical UniVersity, Pr Lenina, 28, 400131 Volgograd, Russia
    J Med Chem 51:4641-52. 2008
    ..These findings were at least in part rationalized by the description of a fair superimposition between the 6-8 and TNK-651 (a HEPT analogue) binding modes in both WT and Y181C RTs...
  69. doi request reprint Identification of long chain alkylidenemalonates as novel small molecule modulators of histone acetyltransferases
    Gianluca Sbardella
    Dipartimento di Scienze Farmaceutiche, Universita degli Studi di Salerno, Via Ponte Don Melillo, 84084 Fisciano SA, Italy
    Bioorg Med Chem Lett 18:2788-92. 2008
    ..The remarkable apoptotic effect together with the ability to selectively acetylate histone versus non-histone substrates appoint 1b as a lead for the development of anticancer drugs...
  70. ncbi request reprint Nitric oxide modulates chromatin folding in human endothelial cells via protein phosphatase 2A activation and class II histone deacetylases nuclear shuttling
    Barbara Illi
    Laboratorio di Biologia Vascolare e Terapia Genica, Centro Cardiologico Fondazione I Monzino, IRCCS, Milan, Italy
    Circ Res 102:51-8. 2008
    ..The present results show that NO-dependent PP2A activation plays a key role in class II HDACs nuclear translocation...
  71. ncbi request reprint Histone deacetylase inhibitors may reduce pathogenicity and virulence in Candida albicans
    Giovanna Simonetti
    Department of Public Health Sciences, University of Rome La Sapienza, Rome Italy
    FEMS Yeast Res 7:1371-80. 2007
    ..These results suggest that selective and specific HDACi could prove to be a valid approach for selected at-risk patients in the combined treatment of infections caused by C. albicans...
  72. ncbi request reprint Slow-, tight-binding HIV-1 reverse transcriptase non-nucleoside inhibitors highly active against drug-resistant mutants
    Reynel Cancio
    Istituto di Genetica Molecolare, Consiglio Nazionale delle Ricerche via Abbiategrasso 207, 27100 Pavia, Italy
    ChemMedChem 2:445-8. 2007
  73. pmc Quinoline derivative MC1626, a putative GCN5 histone acetyltransferase (HAT) inhibitor, exhibits HAT-independent activity against Toxoplasma gondii
    Aaron T Smith
    Department of Pharmacology and Toxicology, IU Center For AIDS Research, Indiana University School of Medicine, 635 Barnhill Drive, MS A 525, Indianapolis, IN 46202, USA
    Antimicrob Agents Chemother 51:1109-11. 2007
    ..However, MC1626 does not inhibit Toxoplasma GCN5 HATs or reduce HAT-mediated activity; rather, this quinoline may target the plastid organelle called the apicoplast...
  74. pmc Histone deacetylase inhibitors and hemoglobin F induction in beta-thalassemia
    Anna Rita Migliaccio
    Division of Hematology Oncology, Department of Medicine, Mount Sinai School of Medicine, One Gustave L Levy Place, New York, NY 10029, USA
    Int J Biochem Cell Biol 40:2341-7. 2008
    ....
  75. ncbi request reprint Role of endogenous reverse transcriptase in murine early embryo development
    Carmine Pittoggi
    Istituto Superiore di Sanita, Rome, Italy
    Mol Reprod Dev 66:225-36. 2003
    ..These results support the conclusion that an endogenous RT activity is required in mouse early embryogenesis specifically between the late 1-cell and the 4-cell stage...
  76. ncbi request reprint Synthesis and in vitro antimycobacterial activity of novel 3-(1H-pyrrol-1-yl)-2-oxazolidinone analogues of PNU-100480
    Gianluca Sbardella
    Dipartimento di Scienze Farmaceutiche, Universita degli Studi di Salerno, Via Ponte Don Melillo, 84084 Fisciano SA, Italy
    Bioorg Med Chem Lett 14:1537-41. 2004
    ..The new derivatives were tested against atypical mycobacteria as well as against drug resistant Mycobacterium tuberculosis and some of them exhibited a fairly good activity against Mycobacterium avium complex (MAC)...