All content © Simona Rapposelli

Designed by Massimiliano Runfola


97.  Sestito S, Pruccoli L, Runfola M, Citi V, Martelli A, Saccomanni G, Calderone V, Tarozzi A, Rapposelli S.. Design and synthesis of H2S-donor hybrids: A new treatment for Alzheimer's disease? (2019)  Eur J Med Chem. 184:111745;.

DOI: 10.1016/j.ejmech.2019.111745

96.  Rogowski M,  Bellusci L,  Sabatini M,  Rapposelli S,  Rahman SM,  Chiellini G, Assadi-Porter FM. Lipolytic Effects of 3-Iodothyronamine (T1AM) and a Novel Thyronamine-Like Analog SG-2 through the AMPK Pathway (2019)  Int. J. Mol. Sci. 20, 4054;.

DOI: 10.3390/ijms20164054

95.  Emmanouilidi A, Fyffe CA, Ferro R, Edling CE, Capone E, Sestito S, Rapposelli S, Lattanzio R, Iacobelli S, Sala G, Maffucci T, Falasca M. Preclinical validation of 3-phosphoinositide-dependent protein kinase 1 inhibition in pancreatic cancer. (2019)  J Exp Clin Cancer Res 38(1):191. DOI: 10.1186/s13046-019-1191-2.

94.  Oliveira LC, Marques MP, Caseiro AJ, Rapposelli S, Batista-de-Carvalho AL, Fonseca AP. A novel approach in glioblastoma multiforme drug discovery: perturbation studies in vitro. (2019)  J Appl Pharm Sci 9(04):058–065.

DOI: 10.7324/JAPS.2019.90407.

93.  Sestito S, Wang S, Chen Q, Lu J, Bertini S, Pomelli C, Chiellini G, He X, Pi R, Rapposelli S. Multi-targeted ChEI-copper chelating molecules as neuroprotective agents. (2019)  Eur J Med Chem 174:216-225.

DOI: 10.1016/j.ejmech.2019.04.060.

92.  Sestito S,  Rapposelli S. A patent update on PDK1 inhibitors (2015-present). (2019)  Expert Opinion on Therapeutic Patents. 29(4):271-82..

DOI: 10.1080/13543776.2019.1597852


91.  Sestito S, Daniele S, Pietrobono D, Citi V, Bellusci L, Chiellini G, Calderone V, Martini C, Rapposelli S. Memantine prodrug as a new agent for Alzheimer's Disease. (2019)  Sci Rep.;9(1):4612.

DOI: 10.1038/s41598-019-40925-8


90.  Alcaro S, Bolognesi ML,  García-Sosa AT,  Rapposelli S. Editorial: Multi-Target-Directed Ligands (MTDL) as Challenging Research Tools in Drug Discovery: From Design to Pharmacological Evaluation. (2019)  Frontiers in Chemistry 7:71

DOI: 10.3389/fchem.2019.00071

89. Salehi B, Sestito S, Rapposelli S, Peron G, Calina D, Sharifi-Rad M, Sharopov F, Martins N, Sharifi-Rad J. Epibatidine: A Promising Natural Alkaloid in Health. (2018) Biomolecules;9(1). pii: E6.

DOI: 10.3390/biom9010006.


88. Nyein C M,  Zhong X, Lu J, Luo H, Wang J, Rapposelli S, Li M,  Ou-yang Y, Pi R, He X. Synthesis and anti-glioblastoma effects of artemisinin-isothiocyanate derivatives. (2018) RSC Advances 8 (71), pp. 40974-40983.

DOI: 10.1039/C8RA08162J


87 Sestito S, Runfola M, Tonelli M, Chiellini G, Rapposelli S. New multitarget approaches in the war against Glioblastoma: a mini-perspective (2018) Front. Pharmacol. 9:874.

DOI: 10.3389/fphar.2018.00874

86 Zhang X, He X, Chen Q, Lu J, Rapposelli S, Pi R. A review on the hybrids of hydroxycinnamic acid as multi-target-directed ligands against Alzheimer's disease (2018) Bioorganic and Medicinal Chemistry, 26 (3), pp. 543-550

DOI: 10.1016/j.bmc.2017.12.042

85. Bellusci L, Laurino A, Sabatini M, Sestito S, Lenzi P, Raimondi L, Rapposelli S, Biagioni F, Fornai F, Salvetti A, Rossi L, Zucchi R, Chiellini G. New insights into the potential roles of 3-Iodothyronamine (T1AM) and newly developed thyronamine-like TAAR1 agonists in neuroprotection (2017) Frontiers in Pharmacology, 8

DOI: 10.3389/fphar.2017.00905

84. Sestito S, Nesi G, Pi R, Macchia M, Rapposelli S. Hydrogen sulfide: a worthwhile tool in the design of new multitarget drugs. (2017) Frontiers in chemistry 5, 72


83. Nesi G, Chen Q, Sestito S, Digiacomo M, Yang X, Wang S, Pi R, Rapposelli S. Nature-based molecules combined with rivastigmine: A symbiotic approach for the synthesis of new agents against Alzheimer's disease. (2017) BIOORG. MED. CHEM. LETTERS 27(21) pp.4812-6

DOI: 10.1016/j.ejmech.2017.10.006

82. Bertini S, Ghilardi E, Asso V, Minutolo F, Rapposelli S, Digiacomo M, Saccomanni G, Salmaso V, Sturlese M, Moro S. Sulfonamido-derivatives of unsubstituted carbazoles as BACE1 inhibitors. (2017) Eur. J. Med Chem, 141, pp.232-239.

DOI: 10.1016/j.bmcl.2017.09.058

81. Nesi G, Sestito S, Digiacomo M, Rapposelli S. Oxidative stress, mitochondrial abnormalities and proteins deposition: multitarget approaches in Alzheimer's disease. (2017) Current topics in medicinal chemistry. 17(27), pp. 3062-79.

DOI: 10.2174/1568026617666170607114232


80. Rapposelli S, Gambari L, Digiacomo M, Citi V, Lisignoli G, Manferdini C, Calderone V, Grassi F. A Novel H2S-releasing Amino-Bisphosphonate which combines bone anti-catabolic and anabolic functions (2017) Scientific Reports, 7 (1), art. no. 11940

DOI: 10.1038/s41598-017-11608-z

79. Daniele S, Sestito S, Pietrobono D, Giacomelli C, Chiellini G, Di Maio D, Marinelli L, Novellino E, Martini C, Rapposelli S. Dual Inhibition of PDK1 and Aurora Kinase A: An Effective Strategy to Induce Differentiation and Apoptosis of Human Glioblastoma Multiforme Stem Cells. ACS Chem Neurosci. 2017 Jan 18;8(1):100-114.

DOI: 10.1021/acschemneuro.6b00251.

78. Digiacomo M, Sartini S, Nesi G, Sestito S, Coviello V, La Motta C, Rapposelli S. Synthesis and Functional Evaluation of Novel Aldose Reductase Inhibitors Bearing a Spirobenzopyran Scaffold. Open Med Chem J. 2017 Jan 31;11:9-23.

DOI: 10.2174/1874104501711010009

77. Chen Z, Digiacomo M, Tu Y, Gu Q, Wang S, Yang X, Chu J, Chen Q, Han Y, Chen J, Nesi G, Sestito S, Macchia M, Rapposelli S, Pi R, Discovery of novel rivastigminehydroxycinnamic acid hybrids as multi-targeted agents for Alzheimer's disease, European Journal of Medicinal Chemistry 2017 Jan 5;125:784-792.

DOI: 10.1016/j.ejmech.2016.09.052


76. Chiellini G, Nesi G, Sestito S, Chiarugi S, Runfola M, Espinoza S, Sabatini M, Bellusci L, Laurino A, Cichero E, Gainetdinov RR, Fossa P, Raimondi L, Zucchi R, Rapposelli S. Hit-to-lead optimization of mouse Trace Amine Associated Receptor 1 (mTAAR1) agonists with a diphenylmethane-scaffold: Design, Synthesis, and biological study. J Med Chem. 2016 Oct 12.

DOI: 10.1021/acs.jmedchem.6b01092


75. Gonca E, Rapposelli S, Darıcı F, Digiacomo M, Yılmaz Z. Antiarrhythmic activity of a new spiro-cyclic benzopyran activator of the cardiac mitochondrial ATP dependent potassium channels. Arch Pharm Res. 2016 Sep;39(9):1212-22.

DOI: 10.1007/s12272-016-0779-8

74.  Petroni D, Bartoli A, Rapposelli S, Digiacomo M, Burchielli S, Nesi G, Lapucci A, Pardini S, Fucci S, Macchia M, Salvadori PA, Menichetti L. Synthesis and In Vivo Imaging of N-(3-[11C]Methoxybenzyl)-2-(3-Methoxyphenyl)ethylaniline as a Potential Targeting Agent for P-glycoprotein. Mol Imaging Biol. 2016 May 27.

DOI: 10.1007/s11307-016-0965-6

73. Sestito S, Daniele S, Nesi G, Zappelli E, Di Maio D, Marinelli L, Digiacomo M, Lapucci A, Martini C, Novellino E, Rapposelli S. Locking PDK1 in DFG-out conformation through 2-oxo-indole containing molecules: Another Tools to Fight Glioblastoma European Journal of Medicinal Chemistry  (2016), 118, 47-63

DOI: 10.1016/j.ejmech.2016.04.003

72. Sestito S, Nesi G, Daniele S, Martelli A, Digiacomo M, Borghini A, Pietra D, Calderone V, Lapucci A, Falasca M, Parrella P, Breschi M, Macchia M, Martini C, Rapposelli S. (2015) Design and synthesis of 2-oxindole multi-targeted inhibitors of PDK1/Akt Signaling Pathway for the treatment of Glioblastoma multiforme European journal of medicinal chemistry, 105:274-288

DOI: 10.1016/j.ejmech.2015.10.020

71. Chiellini G, Nesi G, Digiacomo M, Malvasi R, Espinoza S, Sabatini M, Frascarelli S, Laurino A, Cichero E, Macchia M, Gainetdinov RR, Fossa P, Raimondi L, Zucchi R, Rapposelli S. (2015) Design, Synthesis, and Evaluation of Thyronamine Analogues as Novel Potent Mouse Trace Amine Associated Receptor 1 (mTAAR1) Agonists. J Med Chem.58(12):5096-107.

DOI: 10.1021/acs.jmedchem.5b00526.


70. Daniele S, Costa B, Zappelli E, Da Pozzo E, Sestito S, Nesi G, Campiglia P, Marinelli L, Novellino E, Rapposelli S, Martini C (2015) Combined inhibition of AKT/mTOR and MDM2 enhances Glioblastoma Multiforme cell apoptosis and differentiation of cancer stem cells. Sci Rep. (5):9956.

DOI: 10.1038/srep09956

69. Digiacomo M,  Chen Z, Wang S, Lapucci A, Macchia M, Yang X, Chu J, Han Y, Pi R, Rapposelli S. (2015) Synthesis and pharmacological evaluation of multifunctional tacrine derivatives against several disease pathways of AD Bioorg Med Chem Lett. 25, 807-810

DOI: 10.1016/j.bmcl.2014.12.084

68. Testai L, Rapposelli S, Martelli A, Breschi MC, Calderone V. Mitochondrial potassium channels as pharmacological target for cardioprotective drugs (2015) Medicinal Research Reviews 35 (3) pp. 520 – 553

DOI: 10.1002/med.21332

67. Digiacomo M, Martelli A, Testai L, Lapucci A, Breschi MC,  Calderone V, Rapposelli S. (2015). Synthesis and evaluation of multi-functional NO-donor/ insulin-secretagogue derivatives for the treatment of type II diabetes and its cardiovascular complications. Bioorg Med Chem 23, 422-428

DOI: 10.1016/j.bmc.2014.12.043

66. Nesi G, Colabufo NA, Contino M, Perrone MG, Digiacomo M, Perrone R, Lapucci A, Macchia M, Rapposelli S. (2014). SAR study on arylmethyloxyphenyl scaffold: Looking for a P-gp nanomolar affinity. Eur. J. Med Chem. 76:558-566

DOI: 10.1016/j.ejmech.2014.02.051

65. Nesi G, Sestito S, Mey V, Ricciardi S, Falasca M, Danesi R, Lapucci A, Breschi MC, Fogli S, Rapposelli S. (2013) Synthesis of Novel 3,5-Disubstituted-2-oxindole Derivatives As Antitumor Agents against Human Nonsmall Cell Lung Cancer ACS Medicinal Chemistry Letters, 4 (12):1137–1141

DOI: 10.1021/ml400162g

64. Martelli A, Testai L, Citi V, Marino A, Pugliesi I, Barresi E, Nesi G, Rapposelli S, Taliani S, Da Settimo F, Breschi MC, Calderone V. (2013) Arylthioamides as H2S Donors: L-​Cysteine-​Activated Releasing Properties and Vascular Effects in Vitro and in Vivo ACS Medicinal Chemistry Letters 4(10):904-908

DOI: 10.1021/ml400239a

63. Zhu D, Chen M, Li M, Luo B, Zhao Y, Huang P, Xue F, Rapposelli S, Pi R, Wen S. (2013) Discovery of novel N-substituted carbazoles as neuroprotective agents with potent anti-oxidative activity. Eur J Med Chem. 68C:81-88.

DOI: 10.1016/j.ejmech.2013.07.029


62. Huang W-Y, Chao X-J, Ouyang Y, Liu A-M, He X-X, Chen M-H, Wang L-H, Liu J, Yu S-W, Rapposelli S, Pi R (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 Neurosciences and Therapeutics 18:950-952.

DOI: 10.1111/cns.12286

61. Chao XJ, He XX, Yang YL, Zhou X, Jin MH, Liu S, Cheng ZY, Liu PQ, Wang YT, Yu JC, Tan Y, Huang YJ, Qin J, Rapposelli S, Pi RB (2012). Design, synthesis and pharmacological evaluation of novel tacrine-caffeic acid hybrids as multi-targeted compounds against Alzheimer's disease. Bioorg. Med. Chem Lett.,  22:6498-6502

DOI: 10.1016/j.bmcl.2012.08.036

60. Rapposelli S, Coi A, Imbriani M, Bianucci AM (2012). Development of classification models for identifying "true" P-glycoprotein (P-gp) inhibitors through inhibition, ATPase activation and monolayer efflux assays. International Journal of Molecular Sciences, 13:6924-6943.

DOI: 10.3390/ijms13066924


59. Chiellini G, Rapposelli S, Zhu J, Massarelli I, Saraceno M, Bianucci AM, Plum LA., Clagett-Dame M, DeLuca H F. (2012), Synthesis and biological activities of vitamin D-like inhibitors of CYP24 hydroxylase. Steroids, 77(3): 212-23.

DOI: 10.1016/j.steroids.2011.11.007

58. Rapposelli S, Da Settimo F, Digiacomo M, La Motta C, Lapucci A, Sartini S, Vanni M. (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(6), 372-385

DOI: 10.1002/ardp.201000302

57. Rapposelli S. (2011)  The Importance of Stereochemistry in Medicinal Chemistry and Drug Discovery. Curr Top Med Chem. 11(7); 758-759 (Editorial)

DOI: 10.2174/156802611795165179

56. Rapposelli S. (2011) Novel ATP-sensitive potassium channel ligands: a patent overview (2005-2010).  Expert Opinion on therapeutic patents, 21(3), 355-379.  

DOI: 10.1517/13543776.2011.553601

55. Rapposelli S, Breschi MC, Calderone V, Digiacomo M, Martelli A, Testai L, Vanni M, Balsamo A. (2011) Synthesis and biological evaluation of 5-membered spiro heterocycle-benzopyran derivatives against myocardial ischemia. European Journal of Medicinal Chemistry  ,  46(3),  966-973.

DOI: 10.1016/j.ejmech.2011.01.003

54. Coi A, Bianucci AM, Rapposelli S, Balsamo A. (2010),  Classification models for the identification of P-gp inhibitors. Drugs of the Future, 35(suppl. A), abstract


53. Rapposelli S, Digiacomo M, Franchi S, Moretti S, Pinza  M, Sacerdote P, Balsamo A. (2010),  Sodium N-(methylsulfonyl)-N-(4-nitro-2-phenoxyphenyl)sulfamate: a water-soluble nimesulide prodrug for parenteral use. Molecular Pharmaceutics, 7(5), 1871–1876,

DOI: 10.1021/mp1001137

52. Calderone V, Testai L, Martelli A, Rapposelli S, Digiacomo M, Balsamo A, Breschi MC (2010), Anti-ischemic properties of a new spiro-cyclic benzopyran activator of the cardiac mitoKATP channel. Biochem. Pharmacol. 79, 39-47

DOI: 10.1016/j.bcp.2009.07.017

51. Rapposelli S, Calderone V, Digiacomo M, Martelli A, Minutolo F, Testai L, Balsamo A. (2009) Spiro-benzopyran structure: a new scaffold for cardioprotection. Drugs of the future, 34 (suppl A), 73 (Abstract).

50. Calderone V, Rapposelli S, Martelli A, Digiacomo M, Testai L, Torri S, Marchetti P, Breschi MC, Balsamo A. (2009), NO-glibenclamide derivatives: Prototypes of a new class of nitric oxide-releasing anti-diabetic drugs. Bioorg. Med. Chem. 17 5426–5432

DOI: 10.1016/j.bmc.2009.06.049

49. Coi A, Bianucci AM, Calderone V, Testai L, Digiacomo M, Rapposelli S, Balsamo A. (2009) Predictive models, based on classification algorithms, for compounds potentially active as mitochondrial ATP-sensitive potassium channel openers Bioorg. Med. Chem. 17 5565–5571.

DOI: 10.1016/j.bmc.2009.06.028

48. Rapposelli S, Calderone V, Cirilli R, Digiacomo M, Faggi C, La Torre F, Manganaro M, Martelli A., Testai L. (2009),  Enantioselectivity in Cardioprotection induced by (S)-(−)-2,2-Dimethyl-N-(4′-acetamido-benzyl)-4-spiromorpholone-chromane J. Med. Chem. 2(5), 1477-1480.

DOI: 10.1021/jm801459f

47. Rapposelli S, Digiacomo M, Balsamo A. (2009), P-gp Transporter and its Role in Neurodegenerative Diseases. Curr Top Med Chem. 9(1), 209-17.

DOI: 10.2174/156802609787521544

46. Minutolo F, Bertini S, GranchiC, Marchitiello T, Prota G, Rapposelli S, Tuccinardi T, Martinelli A, Gunther JR, Carlson KE, Katzenellenbogen JA, Macchia M. (2009) Structural Evolutions of Salicylaldoximes as Selective Agonists for Estrogen Receptor b.  J. Med. Chem.,  52(3), 858-867

DOI: 10.1021/jm801458t

45. Colabufo NA, Berardi F, Perrone R, Rapposelli S, Digiacomo M, Vanni M, Balsamo A. (2008) 2-[(3-Methoxyphenylethyl)phenoxy]-based ABCB1 inhibitors: effect of different basic side-chains on their biological properties. J. Med. Chem., 51(23), 7602-7613

DOI: 10.1021/jm800928j

44. Breschi MC, Calderone V, Digiacomo M, Manganaro M, Martelli A, Minutolo F, Rapposelli S, Testai L, Tonelli F, Balsamo A. (2008), Spirocyclic Benzopyran-based derivatives as new anti-ischemic activators of mitochondrial ATP-sensitive potassium channel. J. Med. Chem. 51(21), 6945-6954.

DOI: 10.1021/jm800956g

43. Asso V, Ghilardi E, Bertini S, Digiacomo M, Granchi C, Minutolo F, Rapposelli S, Bartolato A, Moro S, Macchia M. (2008) Alpha-Naphthylaminopropan-2-ol derivatives as BACE1 inhibitors. ChemMedChem  ,  3(10),  1530-1534.

DOI: 10.1002/cmdc.200800162

42. Torri S, Galli M, Calderone V, Rapposelli S, Digiacomo M, Martelli A, Lupi R, Del Guerra S, Bugliani M, Mancarella R, D'Aleo V, Boggi U, Balsamo A. (2008) Pharmacodynamic hybrids with insulin secretagogue and NO-Donor activity. DIABETES 57, A584, abstract (ISSN 0012-1797)

41. Rapposelli S, Cuboni S, Digiacomo M, Lucacchini A,  Minutolo F, Trincavelli ML, Balsamo, A. (2008) Synthesis and Affinity Evaluation for AT1 Receptor of Phenylsalicylaldoxime-Derivatives Structurally Related to Sartans, Heterocycles, 75(6), 1467-1478

DOI: 10.3987/COM-07-11309

40. Rapposelli S, Cuboni S, Digiacomo M.; Lapucci, A.; Trincavelli, Maria L.; Tuccinardi, T.; Balsamo, A. (2008) Synthesis and AT1 affinity evaluation of benzamidophenyl analogs of known AT1 receptor ligands with similar aromatic skeleton  ARKIVOC (Gainesville, FL, United States), ii, 268-286

39. Minutolo F, Bellini R, Bertini S, Carboni I, Lapucci A, Pistolesi L, Prota G, Rapposelli S, Solati F, Tuccinardi T, Martinelli A, Stossi F, Carlson KE, Katzenellenbogen BS, Katzenellenbogen JA, Macchia M. (2008) Monoaryl-Substituted Salicylaldoximes as Ligands for Estrogen Receptor J. Med. Chem., 51, 1344–1351

DOI: 10.1021/jm701396g

38. Colabufo NA, Berardi F,  Perrone R, Rapposelli S, Digiacomo M, Vanni M, Balsamo A. (2008) Synthesis and Biological Evaluation of (Hetero)Arylmethyloxy- and Arylmethylamine-phenyl Derivatives as Potent P-glycoprotein Modulating Agents. J. Med. Chem. 51, 1415-1422.

DOI: 10.1021/jm701267q

37. Calderone V, Digiacomo M, Martelli A, Minutolo F, Rapposelli S, Testai L, Balsamo A. (2008) Evaluation of the NO-releasing properties of NO-donor linkers  J.Pharm.Pharmacol., 60(2), 189-195

DOI: 10.1211/jpp.60.2.0007

36. Balsamo A, Calderone V, Rapposelli S. (2008) New Emerging Prospects in the Pharmacotherapy of Hypertension  Cardiovasc Hematol Agents Med Chem., 6(1), 1-19. Review.

DOI: 10.2174/187152508783329993

35. Torri S, Galli M, Calderone V, Rapposelli S, Digiacomo M, Martelli A, D'Aleo V, Boggi U, Balsamo A, Marchetti P.(2007) In-vitro evaluation of new pharmacodynamic hybrids with insulin secretagogue and NO-donor activity DIABETOLOGIA 50, S374, abstract (ISSN 0012-186X)

34. Calderone V, Testai L, Martelli A, Rapposelli S, Breschi MC. (2007) Activators of cardiac mitochondrial ATP-sensitive potassium channels: promising drugs for anti-ischaemic therapy. Curr Topics Pharmacol., 11(1), 81-90. Review

33. Orlandini E, Rapposelli S, Nencetti S, Giannaccini G, Betti L, Balsamo A. (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 (Weinheim), 340(3), 135-139.

DOI: 10.1002/ardp.200600123

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

DOI: 10.2174/187152507779315831

31. Breschi MC, Calderone V, Martelli A, Minutolo F, Rapposelli S, Testai L, Tonelli F, Balsamo A. (2006) New benzopyran-based openers of the mitochondrial KATP potassium channel with potent anti-ischaemic properties. J. Med. Chem.,  49, 7600-7602.

DOI: 10.1021/jm061228l

30. Colabufo NA, Berardi F, Perrone R,  Rapposelli S, Digiacomo M, Balsamo A. (2006) Arylmethyloxyphenyl Derivatives: Small Molecules Displaying P-Glycoprotein Inhibition. J. Med. Chem.  ,  49(22),  6607-6613.

DOI: 10.1021/jm060639z

29. Minutolo F, Bertini S, Martinelli A, Ortore G, Placanica G, Prota G, Rapposelli S, Tuccinardi T, Sheng S, Carlson KE, Katzenellenbogen BS,  Katzenellenbogen JA, Macchia M. (2006) Salicylaldoximes and anthranylaldoximes as alternatives to phenol-based estrogen receptor ligands.    ARKIVOC (Gainesville, FL, United States), 8,  83-94. 

28. Tuccinardi T, Bertini S, Martinelli A, Minutolo F, Ortore G, Placanica G, Prota G, Rapposelli S, Carlson KE, Katzenellenbogen JA, Macchia M. (2006) Synthesis of Anthranylaldoxime Derivatives as Estrogen Receptor Ligands and Computational Prediction of Binding Modes. J. Med. Chem.,  49(16),  5001-5012. 

DOI: 10.1021/jm060560u

27. Tuccinardi T, Calderone V, Rapposelli S, Martinelli A. (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(14),  4305-4316.

DOI: 10.1021/jm060338p

26. Breschi MC, Calderone V, Digiacomo M, Macchia M, Martelli A, Martinotti E, Minutolo F, Rapposelli S, Rossello A, Testai L, Balsamo A.  (2006)  New NO-Releasing Pharmacodynamic Hybrids of Losartan and Its Active Metabolite: Design, Synthesis, and Biopharmacological Properties.  J. Med. Chem.,  49(8),  2628-2639. 

DOI: 10.1021/jm0600186

25. Martelli A, Rapposelli S, Calderone V. (2006) NO-releasing hybrids of cardiovascular drugs.  Curr. Med. Chem.,  13(6),  609-625. 

DOI: 10.2174/092986706776055634

24. Minutolo F, Bertini S, Betti L, Danesi R, Gervasi G, Giannaccini G, Martinelli A, Papini AM, Peroni E, Placanica G, Rapposelli S, Tuccinardi T, Macchia M. (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. ChemMedChem,  1(2),  218-224.

DOI: 10.1002/cmdc.200500010



23. Minutolo F, Sala G, Bagnacani A, Bertini S, Carboni I, Placanica G, Prota G, Rapposelli S, Sacchi N, Macchia M, Ghidoni R.   (2005) Synthesis of a Resveratrol Analogue with High Ceramide-Mediated Proapoptotic Activity on Human Breast Cancer Cells. J.Med. Chem. ,  48(22),  6783-6786.

DOI: 10.1021/jm050528k


22. Minutolo, F, Asso, V, Bertini, S, Betti, L, Ciriaco, M, Danesi, R, Gervasi, G, Ghilardi, E, Giovanetti, E, Giannaccini, G, Placanica, G, Prota, G, Rapposelli S, Macchia, M. (2005)   Variously substituted (phosphonoacetamido)oxy analogues of geranylgeranyl diphosphate (GGdP) as GGdP-transferase (GGTase) inhibitors and antiproliferative agents. Med. Chem.  ,  1(3),  239-244.

DOI: 10.2174/1573406053765512t


21. Rossello A, Nuti E, Catalani MP, Carelli P, Orlandini E, Rapposelli S, Tuccinardi T, Atkinson S.J, Murphy G, Balsamo A. (2005) A new development of matrix metalloproteinase inhibitors: twin hydroxamic acids as potent inhibitors of MMPs. Bioorg. Med. Chem. Lett.,  15(9),  2311-2314.

DOI: 10.1016/j.bmcl.2005.03.002


20. Minutolo F, Antonello M, Barontini S, Bertini S, Betti L, Danesi R, Gervasi G, Giannaccini G, Papi C, Placanica G, Rapposelli S, Macchia M.  Phosphonomethylphosphorylmethyl(oxy)-analogues of geranylgeranyl diphosphate as stable and selective geranylgeranyl protein transferase inhibitors. Farmaco,   59(11),  887-892.

DOI: 10.1016/j.farmac.2004.08.002


19. Minutolo F, Asso V, Bertini S, Betti L, Gervasi G, Ghilardi E, Giannaccini G, Placanica G, Prota G, Rapposelli S, Macchia M. (2004) Stable propylphosphonic acid analogues of geranylgeranyl diphosphate possessing inhibitory activity on geranylgeranyl protein transferase. Farmaco,  59(11),  857-861.  

DOI: 10.1016/j.farmac.2004.06.003


18. Breschi M.C, Calderone V, Digiacomo M, Martelli A, Martinotti E, Minutolo F, Rapposelli S, Balsamo A. (2004) NO-Sartans: A New Class of Pharmacodynamic Hybrids as Cardiovascular Drugs. J. Med. Chem.,  47(23),  5597-5600. 

DOI: 10.1021/jm049681p


17. Rossello A, Orlandini E, Nuti E, Rapposelli S, Macchia M, Di Modugno E, Balsamo A. (2004) Synthesis and antimicrobial activity of new 7b- (benzo[a]dihydrocarbazolyloxyacetyl)-substituted cephalosporins. Farmaco,  59(9),  691-696. 

DOI: 10.1016/j.farmac.2004.05.001


16. Minutolo F, Antonello M, Bertini S, Placanica G, Rapposelli S, Carlson K. E, Katzenellenbogen J. A, Macchia M. (2004) Diaryl-substituted salicyl- and anthranyl-ketoximes as potential estrogen receptor ligands.  Farmaco,  59(8),  601-607. 

DOI: 10.1016/j.farmac.2004.01.007


15. Rossello A, Nuti E, Orlandini E, Carelli P, Rapposelli S, Macchia M, Minutolo F, Carbonaro L, Albini A, Benelli R, Cercignani G, Murphy G, Balsamo A. (2004) New N-arylsulfonyl-N-alkoxyaminoacetohydroxamic acids as selective inhibitors of gelatinase A (MMP-2). Bioorg. Med. Chem.,  12(9),  2441-2450. 

DOI: 10.1016/j.bmc.2004.01.047


14. Rapposelli S, Lapucci A, Minutolo F, Orlandini E, Ortore G, Pinza M, Balsamo A. (2004) Synthesis and COX-2 inhibitory properties of N-phenyl- and N-benzyl-substituted amides of 2-(4-methylsulfonylphenyl)cyclopent-1-ene-1-carboxylic acid and of their pyrazole, thiophene and isoxazole analogs. Farmaco,  59(1),  25-31. 

DOI: 10.1016/j.farmac.2003.09.003


13. Minutolo F, Bertini S, Betti L, Danesi R, Gervasi G, Giannaccini G, Papi C, Placanica G, Barontini S, Rapposelli S, Macchia M. (2003) Stable analogs of geranylgeranyl diphosphate possessing improved geranylgeranyl versus farnesyl protein transferase inhibitory selectivity. Bioorg. Med. Chem. Lett.,  13(24),  4405-4408.

DOI: 10.1016/j.bmcl.2003.09.035


12. Minutolo F, Bertini S, Betti L, Di Bussolo V, Giannaccini G, Placanica G, Rapposelli S, Spielmann H. P, Macchia M. (2003) Synthesis of aniline-type analogues of farnesyl diphosphate and their biological assays for prenyl protein transferase inhibitory activity. Farmaco, 58(12),  1277-1281.  

DOI: 10.1016/j.farmac.2003.08.002


11. Balsamo A, Mancini F, Milanese C, Orlandini E, Ortore G, Pinza M, Rapposelli S, Rossello A. (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(9),  707-714.  

DOI: 10.1016/S0014-827X(03)00110-1


10. Minutolo F, Antonello M, Bertini S, Ortore G, Placanica G, Rapposelli S, Sheng S, Carlson K. E, Katzenellenbogen B. S, Katzenellenbogen J. A, Macchia M. (2003) Novel Estrogen Receptor Ligands Based on an Anthranylaldoxime Structure: Role of the Phenol-Type Pseudocycle in the Binding Process. J. Med. Chem. ,  46(19),  4032-4042.  

DOI: 10.1021/jm0308390


9. Minutolo F, Antonello M, Bertini S, Rapposelli S, Rossello A, Sheng S, Carlson K. E, Katzenellenbogen J. A, Macchia M. (2003)  Synthesis, binding affinity, and transcriptional activity of hydroxy- and methoxy-Substituted 3,4-Diarylsalicylaldoximes on estrogen receptors a  and b. Bioorg. Med. Chem.  11(7),  1247-1257.

DOI: 10.1016/S0968-0896(02)00640-5


8. Macchia M, Bertini S, Fogli S, Giovannetti E, Minutolo F, Rapposelli S, Danesi R. (2003)   Ceramide analogues in apoptosis: a new strategy for anticancer drug development. Farmaco  ,  58(3),  205-211.

DOI: 10.1016/S0014-827X(03)00015-6


7. Balsamo A, Coletta I, Guglielmotti A, Landolfi C, Mancini F, Martinelli A, Milanese C, Minutolo F, Nencetti S, Orlandini E, Pinza M, Rapposelli S, Rossello A. (2003) Synthesis of heteroaromatic analogs 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(2),  157-168.

DOI: 10.1016/S0223-5234(02)01448-4


6. Macchia M, Antonello M, Bertini S, Di Bussolo V, Fogli S, Giovannetti E, Minutolo F, Rapposelli S, Danesi R. (2003) Conformationally restrained ceramide analogues: effects of lipophilic modifications on the antiproliferative activity. Farmaco, 58(1),  85-89. 

DOI: 10.1016/S0014-827X(02)00002-2


5. Rossello, A, Bertini, S, Lapucci, A, Macchia, M, Martinelli, A, Rapposelli, S, Herreros, E, Macchia, B. (2002) Synthesis, Antifungal Activity, and Molecular Modeling Studies of New Inverted Oxime Ethers of Oxiconazole. J. Med. Chem. , 45(22),  4903-4912.

DOI: 10.1021/jm020980t


4. Balsamo, A, Coletta, I, Guglielmotti, A, Landolfi, C, Lapucci, A, Mancini, F, Milanese, C, Minutolo, F, Orlandini, E, Ortore, G, Pinza, M, Rapposelli, S. (2002) Aryl-substituted methyleneaminoxymethyl (MAOM) analogues of diarylcyclopentenyl cyclooxygenase-2 inhibitors: effects of some structural modifications on their biological properties. Eur. J. Med. Chem.,,  37(7),  585-594. 

DOI: 10.1016/S0223-5234(02)01385-5


3. Balsamo, A, Coletta, I, Domiano, P, Guglielmotti, A, Landolfi, C, Mancini, F, Milanese, C, Orlandini, E, Rapposelli, S, Pinza, M, Macchia, B. (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(5),  391-398.

DOI: 10.1016/S0223-5234(02)01359-4


2. Balsamo, A, Bertini, S, Gervasi, G, Lapucci, A, Nencetti, S, Orlandini, E, Rapposelli, S, Rossello, A, Soldani, G. (2001) Enantiopure 3-(arylmethylidene)aminoxy-2-methylpropionic acids: synthesis and antiinflammatory properties. Eur. J. Med. Chem., 36(10),  799-807. 

DOI: 10.1016/S0223-5234(01)01275-2


1. Balsamo A, Cercignani G, Gentili D, Lapucci A, Macchia M, Orlandini E, Rapposelli S, Rossello A. (2001)   Synthesis and inhibitory activity towards human leukocyte elastase of new 7a -methoxy and 7a -chloro(2-acyloxymethyl)cephem derivatives. Eur. J. Med. Chem., 36(2),  185-193.

DOI: 10.1016/S0223-5234(01)01211-9