5 results on '"Bagnarelli L."'
Search Results
2. Cu(I) and Cu(II) Complexes Based on Lonidamine-Conjugated Ligands Designed to Promote Synergistic Antitumor Effects.
- Author
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Del Bello F, Pellei M, Bagnarelli L, Santini C, Giorgioni G, Piergentili A, Quaglia W, Battocchio C, Iucci G, Schiesaro I, Meneghini C, Venditti I, Ramanan N, De Franco M, Sgarbossa P, Marzano C, and Gandin V
- Subjects
- Cell Line, Tumor, Copper chemistry, Copper pharmacology, Crystallography, X-Ray, Humans, Indazoles, Ligands, Molecular Structure, Antineoplastic Agents chemistry, Antineoplastic Agents pharmacology, Coordination Complexes chemistry, Coordination Complexes pharmacology
- Abstract
Bis(pyrazol-1-yl)- and bis(3,5-dimethylpyrazol-1-yl)-acetates were conjugated with the 2-hydroxyethylester and 2-aminoethylamide derivatives of the antineoplastic drug lonidamine to prepare Cu(I) and Cu(II) complexes that might act through synergistic mechanisms of action due to the presence of lonidamine and copper in the same chemical entity. Synchrotron radiation-based complementary techniques [X-ray photorlectron spectroscopy and near-edge X-ray absorption fine structure (NEXAFS)] were used to characterize the electronic and molecular structures of the complexes and the local structure around the copper ion (XAFS) in selected complexes. All complexes showed significant antitumor activity, proving to be more effective than the reference drug cisplatin in a panel of human tumor cell lines, and were able to overcome oxaliplatin and multidrug resistance. Noticeably, these Cu complexes appeared much more effective than cisplatin against 3D spheroids of pancreatic PSN-1 cancer cells; among these, PPh
3 -containing Cu(I) complex 15 appeared to be the most promising derivative. Mechanistic studies revealed that 15 induced cancer cell death by means of an apoptosis-alternative cell death.- Published
- 2022
- Full Text
- View/download PDF
3. Synthesis and Cytotoxic Activity Evaluation of New Cu(I) Complexes of Bis(pyrazol-1-yl) Acetate Ligands Functionalized with an NMDA Receptor Antagonist.
- Author
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Pellei M, Bagnarelli L, Luciani L, Del Bello F, Giorgioni G, Piergentili A, Quaglia W, De Franco M, Gandin V, Marzano C, and Santini C
- Subjects
- Antineoplastic Agents chemical synthesis, Cell Line, Tumor, Cells, Cultured, Coordination Complexes chemical synthesis, Humans, Ligands, Molecular Structure, Acetates chemistry, Antineoplastic Agents chemistry, Antineoplastic Agents pharmacology, Coordination Complexes chemistry, Coordination Complexes pharmacology, Copper chemistry, Pyrazoles chemistry, Receptors, N-Methyl-D-Aspartate agonists
- Abstract
In the present article, copper(I) complexes of bis(pyrazol-1-yl) carboxylic acid (LH), bis(3,5-dimethylpyrazol-1-yl) carboxylic acid (L
2 H), and bis(pyrazol-1-yl) acetates conjugated with an N -methyl-d-aspartate (NMDA) receptor antagonist (LNMDA or L2NMDA ) and phosphane ligands (triphenylphosphine or 1,3,5-triaza-7-phosphaadamantane) were synthesized. The selection of an NMDA antagonist for the coupling with LH and L2 H was suggested by the observation that NMDA receptors are expressed and play a role in different types of cancer models. All the new complexes showed a significant antitumor activity on a panel of human tumor cell lines of different histology, with cisplatin-sensitive, cisplatin-resistant, or multi-drug-resistant phenotype. Their half maximal inhibitory concentration (IC50 ) values were in the low- and sub-micromolar range and, in general, significantly lower than that of cisplatin. Interestingly, the fact that all the complexes proved to be significantly more active than cisplatin even in three-dimensional (3D) spheroids of H157 and BxPC3 cancer cells increased the relevance of the in vitro results. Finally, morphological analysis revealed that the most representative complex 8 induced a massive swelling of the endoplasmic reticulum (ER) membrane, which is a clear sign of ER stress.- Published
- 2020
- Full Text
- View/download PDF
4. Syntheses and biological studies of nitroimidazole conjugated heteroscorpionate ligands and related Cu(I) and Cu(II) complexes.
- Author
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Pellei M, Gandin V, Cimarelli C, Quaglia W, Mosca N, Bagnarelli L, Marzano C, and Santini C
- Subjects
- A549 Cells, Cell Death drug effects, Humans, MCF-7 Cells, Models, Molecular, Molecular Structure, Solubility, Antineoplastic Agents chemical synthesis, Antineoplastic Agents chemistry, Antineoplastic Agents pharmacology, Colonic Neoplasms drug therapy, Colonic Neoplasms metabolism, Colonic Neoplasms pathology, Coordination Complexes chemical synthesis, Coordination Complexes chemistry, Coordination Complexes pharmacology, Copper chemistry, Copper pharmacology, Nitroimidazoles chemistry, Nitroimidazoles pharmacology
- Abstract
Copper(I) and copper(II) complexes of 5-nitroimidazole conjugated heteroscorpionate ligands have been synthesized. In particular, the new 2,2-bis(pyrazol-1-yl)-N-(2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl)acetamide ligand (L
H MN) was synthesized by direct coupling of preformed side chain acid with 5-nitroimidazole and its coordination chemistry was investigated towards Cu(I) and Cu(II) acceptors and compared with that of the related 2,2-bis(3,5-dimethyl-1-H-pyrazol-1-yl)-N-(2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl)acetamide ligand (LMe MN). The copper(II) complexes {[(LMe MN)2 Cu]Cl2 } and {[(LH MN)2 Cu]Cl2 } were prepared by the reaction of CuCl2 ·2H2 O with LH MN or LMe MN ligands in methanol solution. The water soluble copper(I) complexes {[(LMe MN)Cu(PTA)2 ]}(PF6 ) and {[(LH MN)Cu(PTA)2 ]}(PF6 ) were prepared by the reaction of Cu(CH3 CN)4 PF6 and 1,3,5-triaza-7-phosphaadamantane (PTA) with LH MN or LMe MN ligands in acetonitrile solution. The new Cu(I) and Cu(II) complexes as well as the corresponding uncoordinated ligands were evaluated for their cytotoxic activity against 2D monolayer cultures of multiple human cancer cell lines and 3D-cultured HCT-15 colon cancer spheroids. Morphological analysis by Transmission Electron Microscopy (TEM) revealed the induction of a massive cytoplasmic vacuolization consistent with a paraptotic-like cancer cell death., (Copyright © 2018 Elsevier Inc. All rights reserved.)- Published
- 2018
- Full Text
- View/download PDF
5. Cu(I) and Cu(II) Complexes Based on Lonidamine-Conjugated Ligands Designed to Promote Synergistic Antitumor Effects
- Author
-
Fabio Del Bello, Maura Pellei, Luca Bagnarelli, Carlo Santini, Gianfabio Giorgioni, Alessandro Piergentili, Wilma Quaglia, Chiara Battocchio, Giovanna Iucci, Irene Schiesaro, Carlo Meneghini, Iole Venditti, Nitya Ramanan, Michele De Franco, Paolo Sgarbossa, Cristina Marzano, Valentina Gandin, Del Bello, F., Pellei, M., Bagnarelli, L., Santini, C., Giorgioni, G., Piergentili, A., Quaglia, W., Battocchio, C., Iucci, G., Schiesaro, I., Meneghini, C., Venditti, I., Ramanan, N., De Franco, M., Sgarbossa, P., Marzano, C., and Gandin, V.
- Subjects
Tumor ,Crystallography ,Indazoles ,Molecular Structure ,Antineoplastic Agents ,Crystallography, X-Ray ,Ligands ,Cell Line ,Inorganic Chemistry ,Cell Line, Tumor ,Copper ,Humans ,Coordination Complexes ,X-Ray ,copper complexes ,Physical and Theoretical Chemistry - Abstract
Bis(pyrazol-1-yl)- and bis(3,5-dimethylpyrazol-1-yl)-acetates were conjugated with the 2-hydroxyethylester and 2-aminoethylamide derivatives of the antineoplastic drug lonidamine to prepare Cu(I) and Cu(II) complexes that might act through synergistic mechanisms of action due to the presence of lonidamine and copper in the same chemical entity. Synchrotron radiation-based complementary techniques [X-ray photorlectron spectroscopy and near-edge X-ray absorption fine structure (NEXAFS)] were used to characterize the electronic and molecular structures of the complexes and the local structure around the copper ion (XAFS) in selected complexes. All complexes showed significant antitumor activity, proving to be more effective than the reference drug cisplatin in a panel of human tumor cell lines, and were able to overcome oxaliplatin and multidrug resistance. Noticeably, these Cu complexes appeared much more effective than cisplatin against 3D spheroids of pancreatic PSN-1 cancer cells; among these, PPh3-containing Cu(I) complex 15 appeared to be the most promising derivative. Mechanistic studies revealed that 15 induced cancer cell death by means of an apoptosis-alternative cell death.
- Published
- 2022
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