Filippo Minutolo

Summary

Affiliation: University of Pisa
Country: Italy

Publications

  1. doi request reprint Monoaryl-substituted salicylaldoximes as ligands for estrogen receptor beta
    Filippo Minutolo
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Pisa, Italy
    J Med Chem 51:1344-51. 2008
  2. ncbi request reprint Metabolically labile cannabinoid esters: a 'soft drug' approach for the development of cannabinoid-based therapeutic drugs
    F Minutolo
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126, Pisa, Italy
    Bioorg Med Chem Lett 17:4878-81. 2007
  3. doi request reprint Structural evolutions of salicylaldoximes as selective agonists for estrogen receptor beta
    Filippo Minutolo
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    J Med Chem 52:858-67. 2009
  4. doi request reprint Estrogen receptor β ligands: recent advances and biomedical applications
    Filippo Minutolo
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Italy
    Med Res Rev 31:364-442. 2011
  5. ncbi request reprint Novel estrogen receptor ligands based on an anthranylaldoxime structure: role of the phenol-type pseudocycle in the binding process
    Filippo Minutolo
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    J Med Chem 46:4032-42. 2003
  6. ncbi request reprint Synthesis of anthranylaldoxime derivatives as estrogen receptor ligands and computational prediction of binding modes
    Tiziano Tuccinardi
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    J Med Chem 49:5001-12. 2006
  7. ncbi request reprint 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
    Simona Rapposelli
    Dipartimento di Scienze Farmaceutiche, Facolta di Farmacia, Universita di Pisa, Via Bonanno, 6, 56100, Pisa, Italy
    Farmaco 59:25-31. 2004
  8. ncbi request reprint 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
    Aldo Balsamo
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126, Pisa, Italy
    Eur J Med Chem 38:157-68. 2003
  9. ncbi request reprint New NO-releasing pharmacodynamic hybrids of losartan and its active metabolite: design, synthesis, and biopharmacological properties
    Maria C Breschi
    Dipartimento di Psichiatria, Neurobiologia, Farmacologia e Biotecnologie, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    J Med Chem 49:2628-39. 2006
  10. ncbi request reprint Diaryl-substituted salicyl- and anthranyl-ketoximes as potential estrogen receptor ligands
    Filippo Minutolo
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    Farmaco 59:601-7. 2004

Collaborators

Detail Information

Publications51

  1. doi request reprint Monoaryl-substituted salicylaldoximes as ligands for estrogen receptor beta
    Filippo Minutolo
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Pisa, Italy
    J Med Chem 51:1344-51. 2008
    ..The chloro-substituted derivative showed the highest beta affinity and selectivity, and it also proved to be an ERbeta partial agonist with an EC 50 of 11 nM...
  2. ncbi request reprint Metabolically labile cannabinoid esters: a 'soft drug' approach for the development of cannabinoid-based therapeutic drugs
    F Minutolo
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126, Pisa, Italy
    Bioorg Med Chem Lett 17:4878-81. 2007
    ..This may constitute a possible solution to the psychotropic side effects encountered when cannabinoids are therapeutically employed as local analgesic or antiglaucoma agents...
  3. doi request reprint Structural evolutions of salicylaldoximes as selective agonists for estrogen receptor beta
    Filippo Minutolo
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    J Med Chem 52:858-67. 2009
    ..The resulting compound showed the best affinity (K(i) = 7.1 nM) and selectivity for ERbeta over ERalpha. Moreover, in transcription assays, it proved to be a selective and potent ERbeta-full agonist with an EC(50) of 4.8 nM...
  4. doi request reprint Estrogen receptor β ligands: recent advances and biomedical applications
    Filippo Minutolo
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Italy
    Med Res Rev 31:364-442. 2011
    ....
  5. ncbi request reprint Novel estrogen receptor ligands based on an anthranylaldoxime structure: role of the phenol-type pseudocycle in the binding process
    Filippo Minutolo
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    J Med Chem 46:4032-42. 2003
    ..The limited size of this pocket does not allow accommodation of N-substituents larger than a methyl group, which is consistent with the low binding affinity of the N-Et compound 5c...
  6. ncbi request reprint Synthesis of anthranylaldoxime derivatives as estrogen receptor ligands and computational prediction of binding modes
    Tiziano Tuccinardi
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    J Med Chem 49:5001-12. 2006
    ..These analyses suggested a molecular basis for the interaction of these compounds with the ERs and enabled the development of models able to predict the mode of ligand binding...
  7. ncbi request reprint 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
    Simona Rapposelli
    Dipartimento di Scienze Farmaceutiche, Facolta di Farmacia, Universita di Pisa, Via Bonanno, 6, 56100, Pisa, Italy
    Farmaco 59:25-31. 2004
    ..These data have been tentatively explained by a conformational study which indicates that at least the N-phenyl-substituted amides 7a-9a present steric hindrances which may prevent a good interaction with COX-2 active site...
  8. ncbi request reprint 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
    Aldo Balsamo
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126, Pisa, Italy
    Eur J Med Chem 38:157-68. 2003
    ..All the isoxazole derivatives were inactive on both COX isoforms...
  9. ncbi request reprint New NO-releasing pharmacodynamic hybrids of losartan and its active metabolite: design, synthesis, and biopharmacological properties
    Maria C Breschi
    Dipartimento di Psichiatria, Neurobiologia, Farmacologia e Biotecnologie, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    J Med Chem 49:2628-39. 2006
    ..Furthermore, the additional anti-ischemic cardio-protective properties and antiplatelet effects of 4a have been preliminarily investigated...
  10. ncbi request reprint Diaryl-substituted salicyl- and anthranyl-ketoximes as potential estrogen receptor ligands
    Filippo Minutolo
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    Farmaco 59:601-7. 2004
    ....
  11. doi request reprint Salicylaldoxime derivatives as new leads for the development of carbonic anhydrase inhibitors
    Tiziano Tuccinardi
    Dipartimento di Scienze Farmaceutiche, Universita degli Studi di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    Bioorg Med Chem 21:1511-5. 2013
    ..The results herein obtained will allow the development of new CA-inhibitors bearing the salicylaldoxime moiety...
  12. doi request reprint Synthesis of sulfonamide-containing N-hydroxyindole-2-carboxylates as inhibitors of human lactate dehydrogenase-isoform 5
    Carlotta Granchi
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    Bioorg Med Chem Lett 21:7331-6. 2011
    ..Some of these compounds displayed state-of-the-art inhibitory potencies against isoform 5 (K(i) values as low as 5.6 μM) and behaved as competitive inhibitors versus both the substrate and the cofactor...
  13. doi request reprint N-Hydroxyindole-based inhibitors of lactate dehydrogenase against cancer cell proliferation
    Carlotta Granchi
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    Eur J Med Chem 46:5398-407. 2011
    ..Some representative examples were tested against two human pancreatic carcinoma cell lines, and displayed a good anti-proliferative activity, which was even more evident under hypoxic conditions...
  14. ncbi request reprint Phosphonomethylphosphorylmethyl(oxy)-analogues of geranylgeranyl diphosphate as stable and selective geranylgeranyl protein transferase inhibitors
    Filippo Minutolo
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    Farmaco 59:887-92. 2004
    ..In particular, the phosphonomethylphosphorylmethoxy derivative showed the highest inhibition potency, accompanied by a satisfactory GGTase/FTase selectivity...
  15. ncbi request reprint Variously substituted (phosphonoacetamido)oxy analogues of geranylgeranyl diphosphate (GGdP) as GGdP-transferase (GGTase) inhibitors and antiproliferative agents
    Filippo Minutolo
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    Med Chem 1:239-44. 2005
    ..We have also measured the cytotoxicity of these compounds on tumour cell lines with the aim of evaluating their potential anti-proliferative effects...
  16. ncbi request reprint Synthesis, binding affinity, and transcriptional activity of hydroxy- and methoxy-substituted 3,4-diarylsalicylaldoximes on estrogen receptors alpha and beta
    Filippo Minutolo
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126, Pisa, Italy
    Bioorg Med Chem 11:1247-57. 2003
    ....
  17. doi request reprint Spirocyclic benzopyran-based derivatives as new anti-ischemic activators of mitochondrial ATP-sensitive potassium channel
    Maria C Breschi
    Dipartimento di Psichiatria, Neurobiologia, Farmacologia e Biotecnologie, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    J Med Chem 51:6945-54. 2008
    ..Furthermore, these effects were not associated with significant hypotensive and vasorelaxing properties, which represent one of the main limiting factors for the clinical use of nonselective K ATP-openers against myocardial ischemia...
  18. ncbi request reprint Stable propylphosphonic acid analogues of geranylgeranyl diphosphate possessing inhibitory activity on geranylgeranyl protein transferase
    Filippo Minutolo
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    Farmaco 59:857-61. 2004
    ..In one case, an excellent GGTase inhibitory activity was obtained (IC(50) = 39 nM), accompanied by a certain degree of GGTase vs. FTase selectivity...
  19. doi request reprint Synthesis of heterocycle-based analogs of resveratrol and their antitumor and vasorelaxing properties
    Simone Bertini
    Department of Pharmaceutical Sciences, University of Pisa, Via Bonanno 6, 56126 Pisa, Italy
    Bioorg Med Chem 18:6715-24. 2010
    ..Furthermore, the vasorelaxing properties showed a good correlation with the electronic properties measured through the electrostatic molecular potential (ESP)...
  20. pmc Assessing the differential action on cancer cells of LDH-A inhibitors based on the N-hydroxyindole-2-carboxylate (NHI) and malonic (Mal) scaffolds
    Carlotta Granchi
    Dipartimento di Farmacia, Universita di Pisa, Via Bonanno 6, I 56126 Pisa, Italy
    Org Biomol Chem 11:6588-96. 2013
    ....
  21. ncbi request reprint Stable analogues of geranylgeranyl diphosphate possessing improved geranylgeranyl versus farnesyl protein transferase inhibitory selectivity
    Filippo Minutolo
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    Bioorg Med Chem Lett 13:4405-8. 2003
    ..The introduction of small alkyl groups (Me, Et) into the diphosphate mimic moiety caused a further decrease in collateral farnesyl protein transferase (FTase) inhibitory activity, thereby improving GGTase I over FTase selectivity...
  22. ncbi request reprint 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
    Filippo Minutolo
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    ChemMedChem 1:218-24. 2006
    ..Moreover, the biological activities of all the compounds reported herein, in particular the preferential FTase inhibitory activity shown by compound 6, were in good agreement with the results of docking analysis...
  23. doi request reprint Carbazole-containing arylcarboxamides as BACE1 inhibitors
    Simone Bertini
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    Bioorg Med Chem Lett 21:6657-61. 2011
    ..To better understand the structure-activity relationships (SAR) of the new derivatives, a docking study procedure has been applied exploiting different conformational and ionic states of BACE1...
  24. pmc Selective and potent agonists for estrogen receptor beta derived from molecular refinements of salicylaldoximes
    Simone Bertini
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    Eur J Med Chem 46:2453-62. 2011
    ..23 nM for 2c and 1.3 nM for 2d). Furthermore, 2d shows a remarkable functional subtype selectivity, with a β/α transcription potency ratio 50-fold higher than that of estradiol...
  25. ncbi request reprint Synthesis of a resveratrol analogue with high ceramide-mediated proapoptotic activity on human breast cancer cells
    Filippo Minutolo
    Department of Pharmaceutical Sciences, University of Pisa, Via Bonanno 6, 56126 Pisa, Italy
    J Med Chem 48:6783-6. 2005
    ..Here we show that the compound with three hydroxyls and a naphthalene ring is the most effective in triggering apoptosis coupled to the induction of endogenous ceramide in human cancer cells...
  26. doi request reprint BACE1 inhibitory activities of enantiomerically pure, variously substituted N-(3-(4-benzhydrylpiperazin-1-yl)-2-hydroxypropyl) arylsulfonamides
    Simone Bertini
    Department of Pharmaceutical Sciences, University of Pisa, Via Bonanno 6, 56126 Pisa, Italy
    Bioorg Med Chem 18:7991-6. 2010
    ....
  27. doi request reprint Evaluation of the NO-releasing properties of NO-donor linkers
    Vincenzo Calderone
    Dipartimento di Psichiatria, Neurobiologia, Farmacologia e Biotecnologie, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    J Pharm Pharmacol 60:189-95. 2008
    ....
  28. doi request reprint Estrogen receptor ligands: a patent review update
    Ilaria Paterni
    Dipartimento di Farmacia, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy 39 050 2219557 39 050 2219605
    Expert Opin Ther Pat 23:1247-71. 2013
    ..Therapeutic interventions by agents that affect the estrogenic signaling pathway might be useful in the treatment of many dissimilar diseases...
  29. doi request reprint Discovery of N-hydroxyindole-based inhibitors of human lactate dehydrogenase isoform A (LDH-A) as starvation agents against cancer cells
    Carlotta Granchi
    Dipartimento di Scienze Farmaceutiche, Università di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    J Med Chem 54:1599-612. 2011
    ..Moreover, NMR experiments showed that these compounds are able to reduce the glucose-to-lactate conversion inside the cell...
  30. ncbi request reprint Identification of new Fyn kinase inhibitors using a FLAP-based approach
    Giulio Poli
    Department of Pharmacy, University of Pisa, 56126 Pisa, Italy
    J Chem Inf Model 53:2538-47. 2013
    ..These results demonstrate the validity of the methodologies we followed. Furthermore, the five active compounds herein described may be considered as interesting leads for the development of new and more efficient Fyn inhibitors. ..
  31. pmc Small-molecule inhibitors of human LDH5
    Carlotta Granchi
    Dipartimento di Farmacia, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    Future Med Chem 5:1967-91. 2013
    ..The roles of hLDH isoforms will be briefly discussed, and then the inhibitors will be grouped into chemical classes. Furthermore, general pharmacophore features will be emphasized throughout the structural subgroups analyzed. ..
  32. ncbi request reprint Ceramide analogues in apoptosis: a new strategy for anticancer drug development
    Marco Macchia
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    Farmaco 58:205-11. 2003
    ..Recently, several analogs of ceramide, able to pass the cell membrane and then to induce apoptosis, have been developed as a new potential approach in anticancer therapy...
  33. doi request reprint Oxime-based inhibitors of glucose transporter 1 displaying antiproliferative effects in cancer cells
    Tiziano Tuccinardi
    Dipartimento di Farmacia, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    Bioorg Med Chem Lett 23:6923-7. 2013
    ....
  34. ncbi request reprint New benzopyran-based openers of the mitochondrial ATP-sensitive potassium channel with potent anti-ischemic properties
    Maria C Breschi
    Dipartimento di Scienze Farmaceutiche and Dipartimento di Psichiatria, Neurobiologia, Farmacologia e Biotecnologie, Universita di Pisa, Via Bonanno 6, I 56126 Pisa, Italy
    J Med Chem 49:7600-2. 2006
    ..Some of the new compounds (1b, 2b, and 4b) exhibited interesting anti-ischemic properties without affecting significantly the blood pressure parameters...
  35. ncbi request reprint New N-n-propyl-substituted 3-aryl- and 3-cyclohexylpiperidines as partial agonists at the D4 dopamine receptor
    Marco Macchia
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    J Med Chem 46:161-8. 2003
    ....
  36. ncbi request reprint New N-arylsulfonyl-N-alkoxyaminoacetohydroxamic acids as selective inhibitors of gelatinase A (MMP-2)
    Armando Rossello
    Dipartimento di Scienze Farmaceutiche, Universita degli Studi di Pisa, Via Bonanno, 6, 56126 Pisa, Italy
    Bioorg Med Chem 12:2441-50. 2004
    ....
  37. ncbi request reprint Synthesis of aniline-type analogues of farnesyl diphosphate and their biological assays for prenyl protein transferase inhibitory activity
    Filippo Minutolo
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    Farmaco 58:1277-81. 2003
    ..The enzyme inhibition tests performed on FTase and GGTase I show that the newly synthesised compounds based on a combination of the aniline-containing portions with (phosphonoacetamido)oxy groups do not afford potent inhibitors...
  38. ncbi request reprint 4-[6-(Dansylamino)hexylamino]-7-methyl-2-phenyl-1,8-naphthyridine as a new potential fluorescent probe for studying A1-adenosine receptor
    Marco Macchia
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Italy
    Farmaco 57:783-6. 2002
    ....
  39. ncbi request reprint Conformationally restrained ceramide analogues: effects of lipophilic modifications on the antiproliferative activity
    Marco Macchia
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Italy
    Farmaco 58:85-9. 2003
    ..Although a significant antiproliferative activity was maintained in most compounds synthesized, none of them showed any improvement with respect to their 6-ethyl-substituted counterparts...
  40. pmc Anticancer agents that counteract tumor glycolysis
    Carlotta Granchi
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    ChemMedChem 7:1318-50. 2012
    ..Herein we review some of the most relevant antiglycolytic agents that have been investigated thus far for the treatment of cancer...
  41. doi request reprint Curaxins: a new family of non-genotoxic multitargeted anticancer agents
    Valeria Di Bussolo
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6 56126 Pisa, Italy
    ChemMedChem 6:2133-6. 2011
  42. ncbi request reprint Synthesis and antiviral properties of 9-[(2-methyleneaminoxyethoxy)methyl]guanine derivatives as novel Acyclovir analogues
    M Macchia
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Italy
    Farmaco 55:104-8. 2000
    ..Some of the newly synthesized compounds proved to possess a certain activity against HSV-1, albeit lower than that of ACV...
  43. ncbi request reprint Synthesis and dopaminergic properties of the two enantiomers of 3-(3,4-dimethylphenyl)-1-propylpiperidine, a potent and selective dopamine D4 receptor ligand
    B Macchia
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Italy
    Bioorg Med Chem Lett 11:223-6. 2001
    ..Furthermore, the (R)-1 enantiomer proved to be highly selective for D4 receptors with respect to D2-D3 receptors, with a Ki ratio higher than 25,000, while the (S)-1 enantiomer was about 100-fold less selective than the (R)-1 one...
  44. ncbi request reprint Design, synthesis, and characterization of the antitumor activity of novel ceramide analogues
    M Macchia
    Department of Pharmaceutical Sciences, University of Pisa, Via Bonanno 6, 56126 Pisa, Italy
    J Med Chem 44:3994-4000. 2001
    ..In conclusion, the present study demonstrates that the new ceramide analogues 1 and 2 are characterized by in vitro and in vivo antitumor activity and low toxicity...
  45. ncbi request reprint 7-Nitrobenzofurazan (NBD) derivatives of 5'-N-ethylcarboxamidoadenosine (NECA) as new fluorescent probes for human A(3) adenosine receptors
    M Macchia
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    Bioorg Med Chem Lett 11:3023-6. 2001
    ....
  46. ncbi request reprint NO-sartans: a new class of pharmacodynamic hybrids as cardiovascular drugs
    Maria C Breschi
    Dipartimento di Psichiatria, Neurobiologia, Farmacologia e Biotecnologie, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    J Med Chem 47:5597-600. 2004
    ..In vivo, the antihypertensive effects of 2a were similar to those of losartan and captopril...
  47. ncbi request reprint Aryl-substituted methyleneaminoxymethyl (MAOM) analogues of diarylcyclopentenyl cyclooxygenase-2 inhibitors: effects of some structural modifications on their biological properties
    Aldo Balsamo
    Dipartimento di Scienze Farmaceutiche, Facolta di Farmacia, Universita di Pisa, Via Bonanno 6, 56126, Pisa, Italy
    Eur J Med Chem 37:585-94. 2002
    ..This last compound was also assayed in vivo for its antiinflammatory activity by means of the carrageenan-induced paw edema test in rats. No inhibitory effects were detected up to dose of 30 mg kg(-1) orally administered...
  48. doi request reprint QSAR models for predicting enzymatic hydrolysis of new chemical entities in 'soft-drug' design
    I Massarelli
    Department of Chemistry and Industrial Chemistry, University of Pisa, Via Risorgimento 35, 56126 Pisa, Italy
    Bioorg Med Chem 17:3543-56. 2009
    ..The study allowed selecting predictive models enabling the classification of New Chemical Entities with regard to hydrolysis rate, that may be exploited for soft-drug design...
  49. ncbi request reprint Salicylaldoxime moiety as a phenolic "A-Ring" substitute in estrogen receptor ligands
    F Minutolo
    Dipartimento di Scienze Farmaceutiche, , Via Bonanno 6, 56126 Pisa, Italy
    J Med Chem 44:4288-91. 2001
    ..The OH of the oxime function appears to mimic the phenolic OH present in more "classical" ER ligands because the binding reduced when the oxime OH is methylated (2) or absent (3)...
  50. ncbi request reprint Inhibitors of lactate dehydrogenase isoforms and their therapeutic potentials
    C Granchi
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    Curr Med Chem 17:672-97. 2010
    ..This review provides an overview of the LDH inhibitors that have been developed up to now, an analysis of their possible isoform-selectivity, and their therapeutic potentials...
  51. ncbi request reprint N6-isopentenyladenosine arrests tumor cell proliferation by inhibiting farnesyl diphosphate synthase and protein prenylation
    Chiara Laezza
    Istituto di Endocrinologia e Oncologia Sperimentale I E O S, CNR, Bari, Italy
    FASEB J 20:412-8. 2006
    ..Our findings indicate that this isoprenoid end product might be used for antineoplastic therapy, an application emulating that of the lovastatin and/or farnesyl-transferase inhibitors..