Dr. Simona Rapposelli

Assistant Professor
University of Pisa, Italy

Highest Degree
Ph.D. in Medicinal Chemistry from University of Pisa, Italy

My URL
https://livedna.org/39.6168

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Area of Interest:

Chemistry
Myocardial Ischemia
Neurodegenerative Diseases
Alzheimer`s Disease
Medicinal Chemistry

Selected Publications

  1. Zhu, D., M. Chen, M. Li, B. Luo and Y. Zhao et al., 2013. Discovery of novel N-substituted carbazoles as neuroprotective agents with potent anti-oxidative activity. Eur. J. Med. Chem., 68C: 81-88.
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  2. Nesi, G., S. Sestito, V. Mey, S. Ricciardi and M. Falasca et al., 2013. Synthesis of novel 3,5-disubstituted-2-oxindole derivatives as antitumor agents against human nonsmall cell lung cancer. ACS Med. Chem. Lett., 4: 1137-1141.
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  3. Martelli, A., L. Testai, V. Citi, A. Marino and I. Pugliesi et al., 2013. Arylthioamides as H2S donors: l-cysteine-activated releasing properties and vascular effects in vitro and in vivo. ACS Med. Chem. Lett., 4: 904-908.
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  4. Rapposelli, S., A. Coi, M. Imbriani and A.M. Bianucci, 2012. Development of classification models for identifying true P-glycoprotein (P-gp) inhibitors through inhibition, ATPase activation and monolayer efflux assays. Int. J. Mol. Sci., 13: 6924-6943.
    CrossRef  |  PubMed  |  

  5. Huang, W.Y., X.J. Chao, Y. Ouyang, A.M. Liu and X.X. He et al., 2012. Tacrine-6-ferulic acid, a novel multifunctional dimer against Alzheimer's disease, prevents oxidative stress-induced neuronal death through activating Nrf2/ARE/HO-1 Pathway in HT22 cells. CNS Neurosci. Therapeutics, 18: 950-952.
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  6. Chiellini, G., S. Rapposelli, J. Zhu, I. Massarelli and M. Saraceno et al., 2012. Synthesis and biological activities of vitamin D-like inhibitors of CYP24 hydroxylase. Steroids, 77: 212-223.
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  7. Chao, X.J., X.X. He, Y.L. Yang, X. Zhou and M.H. Jin et al., 2012. Design, synthesis and pharmacological evaluation of novel tacrine-caffeic acid hybrids as multi-targeted compounds against Alzheimers disease. Bioorg. Med. Chem. Lett., 22: 6498-6502.
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  8. Rapposelli, S., M.C. Breschi, V. Calderone, M. Digiacomo and A. Martelli et al., 2011. Synthesis and biological evaluation of 5-membered spiro heterocycle-benzopyran derivatives against myocardial ischemia. Eur. J. Med. Chem., 46: 966-973.
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  9. Rapposelli, S., F. da Settimo, M. Digiacomo, C. La Motta, A. Lapucci, S. Sartini and M. Vanni, 2011. Synthesis and Biological Evaluation of 2′-Oxo-2,3-dihydro-3′H- spiro[chromene-4,5′-[1,3]oxazolidin]-3′yl]acetic acid derivatives as aldose reductase inhibitors. Arch. Pharm. (Weinheim), 344: 372-385.
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  10. Rapposelli, S., 2011. The importance of stereochemistry in medicinal chemistry and drug discovery. Curr. Top. Med. Chem., 11: 758-759.

  11. Rapposelli, S., 2011. Novel ATP-sensitive potassium channel ligands: a patent overview (2005-2010). Exp. Opinion Therapeutic Patents, 21: 355-379.

  12. Rapposelli, S., M. Digiacomo, S. Franchi, S. Moretti, M. Pinza, P. Sacerdote and A. Balsamo, 2010. Sodium N-(methylsulfonyl)-N-(4-nitro-2-phenoxyphenyl)sulfamate: a water-soluble nimesulide prodrug for parenteral use. Mol. Pharm., 7: 1871-1876.
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  13. Calderone, V., L. Testai, A. Martelli, S. Rapposelli, M. Digiacomo, A. Balsamo and M.C. Breschi, 2010. Anti-ischemic properties of a new spiro-cyclic benzopyran activator of the cardiac mitoKATP channel. Biochem. Pharmacol., 79: 39-47.
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  14. Rapposelli, S., M. Digiacomo and A. Balsamo, 2009. P-gp transporter and its role in neurodegenerative diseases. Curr. Top. Med. Chem., 9: 209-217.

  15. Rapposelli, S, V. Calderone, R. Cirilli, M. Digiacomo and C. Faggi et al., 2009. Enantioselectivity in Cardioprotection induced by (S)-(−)-2,2-Dimethyl-N-(4′-acetamido-benzyl)-4-spiromorpholone-chromane. J. Med. Chem., 52: 1477-1480.

  16. Minutolo, F., S. Bertini, C. Granchi, T. Marchitiello and G. Prota et al., 2009. Structural evolutions of salicylaldoximes as selective agonists for estrogen receptor β. J. Med. Chem., 52: 858-867.
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  17. Coi, A., A.M. Bianucci, V. Calderone, L. Testai, M. Digiacomo, S. Rapposelli and A. Balsamo, 2009. Predictive models, based on classification algorithms, for compounds potentially active as mitochondrial ATP-sensitive potassium channel openers. Bioorg. Med. Chem., 17: 5565-5571.
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  18. Calderone, V., S. Rapposelli, A. Martelli, M. Digiacomo and L. Testai et al., 2009. NO-glibenclamide derivatives: Prototypes of a new class of nitric oxide-releasing anti-diabetic drugs. Bioorg. Med. Chem., 17: 5426-5432.
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  19. Rapposelli, S., S. Cuboni, M. Digiacomo, A. Lucacchini, F. Minutolo, M.L. Trincavelli and A. Balsamo, 2008. Synthesis and affinity evaluation for at1 receptor of phenylsalicylaldoxime-derivatives structurally related to sartans. Heterocycles, 75: 1467-1478.
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  20. Rapposelli, S., S. Cuboni, M. Digiacomo, A. Lapucci, M.L. Trincavelli, T. Tuccinardi and A. Balsamo, 2008. Synthesis and AT1 affinity evaluation of benzamidophenyl analogs of known AT1 receptor ligands with similar aromatic skeleton. ARKIVOC., 2: 268-286.
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  21. Minutolo, F., R. Bellini, S. Bertini, I. Carboni and A. Lapucci et al., 2008. Monoaryl-substituted salicylaldoximes as ligands for estrogen receptor. J. Med. Chem., 51: 1344-1351.

  22. Colabufo, N.A., F. Berardi, R. Perrone, S. Rapposelli, M. Digiacomo, M. Vanni and A. Balsamo, 2008. Synthesis and biological evaluation of (Hetero)arylmethyloxy- and arylmethylamine-phenyl derivatives as potent P-glycoprotein modulating agents. J. Med. Chem., 51: 1415-1422.

  23. Colabufo, N.A., F. Berardi, R. Perrone, S. Rapposelli, M. Digiacomo, M. Vanni and A. Balsamo, 2008. 2-[(3-Methoxyphenylethyl)phenoxy]-based ABCB1 inhibitors: Effect of different basic side-chains on their biological properties. J. Med. Chem., 51: 7602-7613.
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  24. Calderone, V., M. Digiacomo, A. Martelli, F. Minutolo, S. Rapposelli, L. Testai and A. Balsamo, 2008. Evaluation of the NO-releasing properties of NO-donor linkers. J. Pharm. Pharmacol., 60: 189-195.
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  25. Breschi, M.C., V. Calderone, M. Digiacomo, M. Manganaro and A. Martelli et al., 2008. Spirocyclic Benzopyran-based derivatives as new anti-ischemic activators of mitochondrial ATP-sensitive potassium channel. J. Med. Chem., 51: 6945-6954.
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  26. Balsamo, A., V. Calderone and S. Rapposelli, 2008. New emerging prospects in the pharmacotherapy of hypertension cardiovasc hematol agents. Med. Chem., 6: 1-19.

  27. Asso, V., E. Ghilardi, S. Bertini, M. Digiacomo and C. Granchi et al., 2008. Α-Naphthylaminopropan-2-ol derivatives as BACE1 inhibitors. Chem. Med. Chem., 3: 1530-1534.

  28. Testai, L., S. Rapposelli and V. Calderone, 2007. Cardiac ATP-sensitive potassium channels, a potential target for an anti-ischaemic pharmacological strategy. Cardiovasc. Haematol. Agents Med. Chem., 5: 79-90.

  29. Orlandini, E., S. Rapposelli, S. Nencetti, G. Giannaccini, L. Betti and A. Balsamo, 2007. Synthesis and 5-HT2A, 5-HT1A and alpha1-binding affinities of 2-[2-Hydroxy-3-(pyridin-3-yl-methyl)amino]-, 2-[2-hydroxy-3-(2-pyridin-2-yl-ethyl)amino]- and 2-[2-hydroxy-3-(4-N-methyl-piperazin-1-yl)-amino]propoxybenzaldehyde-O-(substituted) benzyl oximes. Arch. Pharm., 340: 135-139.

  30. Calderone, V., L. Testai, A. Martelli, S. Rapposelli and M.C. Breschi, 2007. Activators of cardiac mitochondrial ATP-sensitive potassium channels: Promising drugs for anti-ischaemic therapy. Curr. Topics Pharmacol., 11: 81-90.

  31. Tuccinardi, T., V. Calderone, S. Rapposelli and A. Martinelli, 2006. Proposal of a new binding orientation for non-peptide AT1 antagonists:  Homology modeling, docking and three-dimensional quantitative structure: Activity relationship analysis. J. Med. Chem., 49: 4305-4316.
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  32. Tuccinardi, T., S. Bertini, A. Martinelli, F. Minutolo and G. Ortore et al., 2006. Synthesis of anthranylaldoxime derivatives as estrogen receptor ligands and computational prediction of binding modes. J. Med. Chem., 49: 5001-5012.
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  33. Minutolo, F., S. Bertini, L. Betti, R. Danesi and G. Gervasi et al., 2006. Synthesis of stable analogues of geranylgeranyl diphosphate possessing a (Z,E,E)-geranylgeranyl side chain, docking analysis, and biological assays for prenyl protein transferase inhibition. Chem. Med. Chem., 1: 218-224.
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  34. Minutolo, F., S. Bertini, A. Martinelli, G. Ortore and G. Placanica et al., 2006. Salicylaldoximes and anthranylaldoximes as alternatives to phenol-based estrogen receptor ligands. Joint Italian-Swiss Med. Chem. Meeting, 8: 83-94.
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  35. Martelli, A., S. Rapposelli and V. Calderone, 2006. NO-releasing hybrids of cardiovascular drugs. Curr. Med. Chem., 13: 609-625.
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  36. Colabufo, N.A., F. Berardi, R. Perrone, S. Rapposelli, M. Digiacomo and A. Balsamo, 2006. Arylmethyloxyphenyl derivatives:  Small molecules displaying P-glycoprotein inhibition. J. Med. Chem., 49: 6607-6613.
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  37. Breschi, M.C., V. Calderone, M. Digiacomo, M. Macchia and A. Martelli et al., 2006. New no-releasing pharmacodynamic hybrids of losartan and its active metabolite:  Design, synthesis and biopharmacological properties. J. Med. Chem., 49: 2628-2639.
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  38. Breschi, M.C., V. Calderone, A. Martelli, F. Minutolo, S. Rapposelli, L. Testai, F. Tonelli and A. Balsamo, 2006. New benzopyran-based openers of the mitochondrial KATP potassium channel with potent anti-ischaemic properties. J. Med. Chem., 49: 7600-7602.

  39. Rossello, A., E. Nuti, M.P. Catalani, P. Carelli and E. Orlandini et al., 2005. A new development of matrix metalloproteinase inhibitors: Twin hydroxamic acids as potent inhibitors of MMPs. Bioorg. Med. Chem. Lett., 15: 2311-2314.
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  40. Minutolo, F., V. Asso, S. Bertini, L. Betti and M. Ciriaco et al., 2005. Variously substituted (phosphonoacetamido)oxy analogues of geranylgeranyl diphosphate (GGdP) as GGdP-transferase (GGTase) inhibitors and antiproliferative agents. Med. Chem., 1: 239-244.
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  41. Minutolo, F., G. Sala, A. Bagnacani, S. Bertini and I. Carboni et al., 2005. Synthesis of a resveratrol analogue with high ceramide-mediated proapoptotic activity on human breast cancer cells. J. Med. Chem., 48: 6783-6786.
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  42. Rossello, A., E. Orlandini, E. Nuti, S. Rapposelli, M. Macchia, E. di Modugno and A. Balsamo, 2004. Synthesis and antimicrobial activity of new 7β-(benzo[a] dihydrocarbazolyloxyacetyl)-substituted cephalosporins. Farmaco, 59: 691-696.
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  43. Rossello, A., E. Nuti, E. Orlandini, P. Carelli and S. Rapposelli et al., 2004. New N-arylsulfonyl-N-alkoxyaminoacetohydroxamic acids as selective inhibitors of gelatinase A (MMP-2). Bioorg. Med. Chem., 12: 2441-2450.

  44. Rapposelli, S., A. Lapucci, F. Minutolo, E. Orlandini, G. Ortore, M. Pinza and A. Balsamo, 2004. Synthesis and COX-2 inhibitory properties of N-phenyl- and N-phenyl-and< i> N-benzyl-substituted amides of 2-(4-methylsulfonylphenyl)cyclopent-1-ene-1-carboxylic acid and of their pyrazole, thiophene and isoxazole analogs. Farmaco, 59: 25-31.
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  45. Minutolo, F., V. Asso, S. Bertini, L. Betti and G. Gervasi et al., 2004. Stable propylphosphonic acid analogues of geranylgeranyl diphosphate possessing inhibitory activity on geranylgeranyl protein transferase. Farmaco, 59: 857-861.
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  46. Minutolo, F., M. Antonello, S. Bertini, G. Placanica and S. Rapposelli et al., 2004. Diaryl-substituted salicyl- and anthranyl-ketoximes as potential estrogen receptor ligands. Farmaco, 59: 601-607.
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  47. Minutolo, F., M. Antonello, S. Barontini, S. Bertini and L. Betti et al., 2004. Phosphonomethylphosphorylmethyl(oxy)-analogues of geranylgeranyl diphosphate as stable and selective geranylgeranyl protein transferase inhibitors. Farmaco, 59: 887-892.
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  48. Breschi, M.C., V. Calderone, M. Digiacomo, A. Martelli and E. Martinotti et al., 2004. NO-sartans:  A new class of pharmacodynamic hybrids as cardiovascular drugs. J. Med. Chem., 47: 5597-5600.
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  49. Minutolo, F., S. Bertini, L. Betti, V. Di Bussolo and G. Giannaccini et al., 2003. Synthesis of aniline-type analogues of farnesyl diphosphate and their biological assays for prenyl protein transferase inhibitory activity. Farmaco, 58: 1277-1281.
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  50. Minutolo, F., S. Bertini, L. Betti, R. Danesi and G. Gervasi et al., 2003. Stable analogs of geranylgeranyl diphosphate possessing improved geranylgeranyl versus farnesyl protein transferase inhibitory selectivity. Bioorg. Med. Chem. Lett., 13: 4405-4408.

  51. Minutolo, F., M. Antonello, S. Bertini, S. Rapposelli and A. Rossello et al., 2003. Synthesis, binding affinity, and transcriptional activity of hydroxy- and methoxy-Substituted 3,4-Diarylsalicylaldoximes on estrogen receptors and Bioorg. Med. Chem., 11: 1247-1257.

  52. Minutolo, F., M. Antonello, S. Bertini, G. Ortore and G. Placanica et al., 2003. Novel estrogen receptor ligands based on an anthranylaldoxime structure: Role of the phenol-type pseudocycle in the binding process. J. Med. Chem., 46: 4032-4042.

  53. Macchia, M., S. Bertini, S. Fogli, E. Giovannetti, F. Minutolo, S. Rapposelli and R. Danesi, 2003. Ceramide analogues in apoptosis: a new strategy for anticancer drug development. Farmaco, 58: 205-211.
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  54. Macchia, M., M. Antonello, S. Bertini, V. Di Bussolo and S. Fogli et al., 2003. Conformationally restrained ceramide analogues: Effects of lipophilic modifications on the antiproliferative activity. Farmaco, 58: 85-89.
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  55. Balsamo, A., I. Coletta, A. Guglielmotti, C. Landolfi and F. Mancini et al., 2003. Synthesis of heteroaromatic analogues of (2-aryl-1-cyclopentenyl-1-alkylidene)-(arylmethyloxy)amine COX-2 inhibitors: Effects on the inhibitory activity of the replacement of the cyclopentene central core with pyrazole, thiophene or isoxazole ring. Eur. J. Med. Chem., 38: 157-168.
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  56. Balsamo, A., F. Mancini, C. Milanese, E. Orlandini and G. Ortore et al., 2003. Synthesis and prostaglandin synthase inhibitory activity of new aromatic O-alkyloxime ethers substituted with methylsulfonamido or methylsulfonyl groups on their aliphatic portion. Farmaco, 58: 707-714.
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  57. Rossello, A., S. Bertini, A. Lapucci, M. Macchia and A. Martinelli et al., 2002. Synthesis, antifungal activity and molecular modeling studies of new inverted oxime ethers of oxiconazole. J. Med. Chem., 45: 4903-4912.
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  58. Balsamo, A., I. Coletta, P. Domiano, A. Guglielmotti and C. Landolfi et al., 2002. (E)-[2-(4-Methylsulphonylphenyl)-1-cyclopentenyl-1-methyliden](arylmethyloxy)amines. Methyleneaminoxymethyl (MAOM) analogues of diarylcyclopentenyl cyclooxygenase-2 inhibitors: Synthesis and biological properties. Eur. J. Med. Chem., 37: 391-398.
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  59. Balsamo, A., I. Coletta, A. Guglielmotti, C. Landolfi and A. Lapucci et al., 2002. Aryl-substituted methyleneaminoxymethyl (MAOM) analogues of diarylcyclopentenyl yclooxygenase-2 inhibitors: Effects of some structural modifications on their biological properties. Eur. J. Med. Chem., 37: 585-594.
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  60. Balsamo, A., S. Bertini, G. Gervasi, A. Lapucci and S. Nencetti et al., 2001. Enantiopure 3-(arylmethylidene)aminoxy-2-methylpropionic acids: Synthesis and antiinflammatory properties. Eur. J. Med. Chem., 36: 799-807.
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  61. Balsamo, A., G. Cercignani, D. Gentili, A. Lapucci and M. Macchia et al., 2001. Synthesis and inhibitory activity towards human leukocyte elastase of new 7-methoxy and 7-chloro(2-acyloxymethyl)cephem derivatives. Eur. J. Med. Chem., 36: 185-193.
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