8 results on '"Banti I"'
Search Results
2. Nuovi derivati piperidinici: sintesi e proprietà biologiche
- Author
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Nencetti, Susanna, Banti, I., Rossello, Armando, Mazzoni, MARIA ROSA, and Lapucci, Annalina
- Published
- 2004
3. In vitro investigation of sulindac derivatives as potential anticancer agents
- Author
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Stefano Fogli, Banti, I., MARIA DIGIACOMO, MARCO MACCHIA, ANNALINA LAPUCCI, and MARIA CRISTINA BRESCHI
4. Identification of histone deacetylase inhibitors with (arylidene)aminoxy scaffold active in uveal melanoma cell lines.
- Author
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Nencetti S, Cuffaro D, Nuti E, Ciccone L, Rossello A, Fabbi M, Ballante F, Ortore G, Carbotti G, Campelli F, Banti I, Gangemi R, Marshall GR, and Orlandini E
- Subjects
- Antineoplastic Agents chemical synthesis, Antineoplastic Agents chemistry, Cell Cycle drug effects, Cell Line, Tumor, Cell Proliferation drug effects, Cell Survival drug effects, Dose-Response Relationship, Drug, Drug Screening Assays, Antitumor, Histone Deacetylase Inhibitors chemical synthesis, Histone Deacetylase Inhibitors chemistry, Humans, Melanoma metabolism, Melanoma pathology, Models, Molecular, Molecular Structure, Quinolines chemical synthesis, Quinolines chemistry, Structure-Activity Relationship, Uveal Neoplasms metabolism, Uveal Neoplasms pathology, Antineoplastic Agents pharmacology, Histone Deacetylase Inhibitors pharmacology, Histone Deacetylases metabolism, Melanoma drug therapy, Quinolines pharmacology, Uveal Neoplasms drug therapy
- Abstract
Uveal melanoma (UM) represents an aggressive type of cancer and currently, there is no effective treatment for this metastatic disease. In the last years, histone deacetylase inhibitors (HDACIs) have been studied as a possible therapeutic treatment for UM, alone or in association with other chemotherapeutic agents. Here we synthesised a series of new HDACIs based on the SAHA scaffold bearing an (arylidene)aminoxy moiety. Their HDAC inhibitory activity was evaluated on isolated human HDAC1, 3, 6, and 8 by fluorometric assay and their binding mode in the catalytic site of HDACs was studied by molecular docking. The most promising hit was the quinoline derivative VS13 , a nanomolar inhibitor of HDAC6, which exhibited a good antiproliferative effect on UM cell lines at micromolar concentration and a capability to modify the mRNA levels of HDAC target genes similar to that of SAHA.
- Published
- 2021
- Full Text
- View/download PDF
5. Synthesis, molecular docking and binding studies of selective serotonin transporter inhibitors.
- Author
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Nencetti S, Mazzoni MR, Ortore G, Lapucci A, Giuntini J, Orlandini E, Banti I, Nuti E, Lucacchini A, Giannaccini G, and Rossello A
- Subjects
- Animals, Humans, Models, Molecular, Neurotransmitter Agents chemical synthesis, Neurotransmitter Agents chemistry, Neurotransmitter Agents pharmacology, Piperidines chemical synthesis, Protein Binding, Rabbits, Serotonin Plasma Membrane Transport Proteins metabolism, Selective Serotonin Reuptake Inhibitors chemical synthesis, Dopamine metabolism, Norepinephrine antagonists & inhibitors, Piperidines chemistry, Piperidines pharmacology, Serotonin metabolism, Selective Serotonin Reuptake Inhibitors chemistry, Selective Serotonin Reuptake Inhibitors pharmacology
- Abstract
With the aim of obtaining compounds possessing high SERT selectivity, in the present work we synthesized and studied the inhibition of serotonin (SERT), dopamine (DAT) and norepinephrine (NET) transporters by docking studies and experimental binding measurements of a series of 4-(aryl)piperidin-3-one O-4-benzyl oxime hydrochlorides (1-10) of both E and Z configuration. E configuration compounds showed high SERT binding affinities (K(i) = 10-98 nM) and high SERT selectivities over both NET and DAT. The molecular docking studies allowed a rationalization of the molecular basis of drug-SERT interactions both of the synthesized compounds and paroxetine and fluoxetine used as reference antidepressant drugs., (Copyright © 2010 Elsevier Masson SAS. All rights reserved.)
- Published
- 2011
- Full Text
- View/download PDF
6. Therapeutic potential of sulindac hydroxamic acid against human pancreatic and colonic cancer cells.
- Author
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Fogli S, Banti I, Stefanelli F, Picchianti L, Digiacomo M, Macchia M, Breschi MC, and Lapucci A
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- Angiogenesis Inhibitors pharmacology, Anti-Inflammatory Agents, Non-Steroidal pharmacology, Caspase 3 metabolism, Caspase 7 metabolism, Cell Line, Tumor, Endothelium, Vascular cytology, Endothelium, Vascular drug effects, Humans, Magnetic Resonance Spectroscopy, Sulindac pharmacology, Anti-Inflammatory Agents, Non-Steroidal therapeutic use, Colonic Neoplasms pathology, Pancreatic Neoplasms pathology, Sulindac therapeutic use
- Abstract
The non-steroidal anti-inflammatory drug (NSAID) sulindac exhibits cyclooxygenase (COX)-dependent and COX-independent chemopreventive properties in human cancer. The present study was aimed at investigating whether the hydroxamic acid substitution for the carboxylic acid group could enhance the in vitro antitumor and antiangiogenic activities of sulindac. Characterization tools used on this study included analyses of cell viability, caspase 3/7 induction, DNA fragmentation, and gene expression. Our findings demonstrate that the newly synthesized hydroxamic acid derivative of sulindac and its sulfone and sulfide metabolites were characterized by a good anticancer activity on human pancreatic and colon cancer cells, both in terms of potency (IC(50) mean values from 6 ± 1.1 μM to 64 ± 1.1 μM) and efficacy (E(max) of ∼100%). Hydroxamic acid derivatives trigger a higher degree of apoptosis than carboxylic acid counterparts, increase bax/bcl-2 expression ratio and induce caspase 3/7 activation. Most notably, these compounds significantly inhibit proangiogenic growth factor-stimulated proliferation of vascular endothelial cell (HUVEC) at sub-micromolar concentrations. Our data also provide evidence that the COX-active metabolite of sulindac hydroxamic acid were the most active of the series and selective inhibition of COX-1 but not COX-2 can mimic its effects, suggesting that COX inhibition could only play a partial role in the mechanism of compound action. In conclusion, these data demonstrate that substitution of the carboxylic acid group with the hydroxamic acid moiety enhances in vitro antiproliferative, proapoptotic and antiangiogenic properties of sulindac, therefore increasing the therapeutic potential of this drug., (Copyright © 2010 Elsevier Masson SAS. All rights reserved.)
- Published
- 2010
- Full Text
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7. Synthesis and in-vitro antitumour activity of new naphthyridine derivatives on human pancreatic cancer cells.
- Author
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Banti I, Nencetti S, Orlandini E, Lapucci A, Breschi MC, and Fogli S
- Subjects
- Antineoplastic Agents administration & dosage, Antineoplastic Agents chemical synthesis, Cell Line, Cell Line, Tumor, Cell Proliferation drug effects, Cell Survival drug effects, Dose-Response Relationship, Drug, Fibroblast Growth Factors administration & dosage, Fluorouracil pharmacology, Humans, Inhibitory Concentration 50, Naphthyridines administration & dosage, Naphthyridines chemical synthesis, Pancreatic Neoplasms pathology, Time Factors, Toxicity Tests, Antineoplastic Agents pharmacology, Apoptosis drug effects, Naphthyridines pharmacology, Pancreatic Neoplasms drug therapy
- Abstract
Objectives: The aim of the study was to evaluate the antitumour effect in vitro of newly synthesized 7-substituted 2,3-dihydro-1,8-naphthyridines., Methods: Characterization tools included cell viability assay, caspase 3/7 induction, DNA fragmentation, fibroblast growth factor type 1 receptor kinase inhibition, and in-vitro antiangiogenic analysis., Key Findings: Treatment of MIA PaCa-2 human pancreatic cancer cells with test compounds showed time- and concentration-dependent cytotoxicity with IC50 values in the micromolar range. Compounds with an aminoalkyl or a diaminoalkyl side chain at the 7-position exhibited remarkable cytotoxicity, whereas the presence of a methyl group or a cyclic amine in the same position led to a significant decrease in their biological activity. Cytotoxicity screening demonstrated that the most active was compound 11 (mean 50% inhibition of cell proliferation (IC50) 11 mum). This compound had an in-vitro antitumour efficacy superior to 5-fluorouracil (the lowest cell viability value after treatment (E(max)) 0.2% and 19%, respectively) and proved to be less toxic than 5-fluorouracil against non-cancerous human oral epithelial cells. In addition, compound 11 induced apoptosis in MIA PaCa-2 cells and it was able to promote antiangiogenic effects in vitro. Finally, its cytotoxicity was enhanced in pancreatic cancer cells stimulated with fibroblast growth factor, while no substantial effect was observed on human bronchial smooth muscle cells stimulated with the same growth factor., Conclusions: These findings suggest that 1,8-naphthyridine derivatives are a promising class of compounds in cancer research. In particular, the antitumour activity of compound 11 is worth further investigation.
- Published
- 2009
- Full Text
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8. 3-[(Aryl)(4-fluorobenzyloxy)methyl]piperidine derivatives: high-affinity ligands for the serotonin transporter.
- Author
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Nencetti S, Demontis GC, Mazzoni MR, Betti L, Banti I, Rossello A, and Lapucci A
- Subjects
- Animals, Antidepressive Agents administration & dosage, Antidepressive Agents chemical synthesis, Binding, Competitive, Cerebral Cortex metabolism, Dose-Response Relationship, Drug, Fluoxetine pharmacology, In Vitro Techniques, Ligands, Piperidines administration & dosage, Piperidines chemical synthesis, Rabbits, Rats, Rats, Wistar, Receptor, Serotonin, 5-HT1A drug effects, Receptors, Adrenergic, alpha-2 metabolism, Serotonin Plasma Membrane Transport Proteins drug effects, Structure-Activity Relationship, Antidepressive Agents pharmacology, Piperidines pharmacology, Receptor, Serotonin, 5-HT1A metabolism, Serotonin Plasma Membrane Transport Proteins metabolism
- Abstract
The structural requirements for high-affinity binding at the serotonin transporter (SERT) have been investigated through the preparation of some 3-[(aryl)(4-fluorobenzyloxy)methyl]piperidine derivatives. The affinity of synthesised piperidinic compounds (1-4) at the SERT was evaluated by displacement of [3H]-paroxetine binding. Derived inhibition constant (Ki) values were in the same order of magnitude as that of fluoxetine, ranging between 2 and 400 nM. To better define the profiles of these compounds as potential antidepressants, binding affinity for 5-HT1A receptors and alpha2-adrenoceptors was also investigated by competition experiments using [3H]8-hydroxy-2-(dipropylamino)tetralin ([3H]8-OH-DPAT) and [3H]rauwolscine as radiolabelled ligands, respectively. Inhibition data indicate that compounds 1-4 possess a very weak affinity for these receptors. The high affinity of compound 1 for SERT indicates that it is worth investigating further.
- Published
- 2007
- Full Text
- View/download PDF
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