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  1. Article ; Online: Synergistic Effects of A Combined Treatment of Glioblastoma U251 Cells with An Anti-miR-10b-5p Molecule and An AntiCancer Agent Based on 1-(3′,4′,5′-Trimethoxyphenyl)-2-Aryl-1 H -Imidazole Scaffold

    Matteo Zurlo / Romeo Romagnoli / Paola Oliva / Jessica Gasparello / Alessia Finotti / Roberto Gambari

    International Journal of Molecular Sciences, Vol 23, Iss 5991, p

    2022  Volume 5991

    Abstract: 1) Background: In the development of new and more effective anticancer approaches, combined treatments appear of great interest. Combination therapy could be of importance in the management of glioblastoma (GBM), a lethal malignancy that accounts for 42% ...

    Abstract (1) Background: In the development of new and more effective anticancer approaches, combined treatments appear of great interest. Combination therapy could be of importance in the management of glioblastoma (GBM), a lethal malignancy that accounts for 42% of cancer of the central nervous system, with a median survival of 15 months. This study aimed to verify the activity on a glioblastoma cancer cell line of one of the most active compounds of a novel series of tubulin polymerization inhibitors based on the 1-(3′,4′,5′-trimethoxyphenyl)-2-aryl-1 H -imidazole scaffold, used in combination with a miRNA inhibitor molecule targeting the oncomiRNA miR-10b-5p. This microRNA was selected in consideration of the role of miR-10b-5p on the onset and progression of glioblastoma. (2) Methods: Apoptosis was analyzed by Annexin-V and Caspase 3/7 assays, efficacy of the anti-miR-10b-5p was assessed by determining the miR-10b-5p content by RT-qPCR. (3) Results: The results obtained show that a “combination therapy” performed by combining the use of an anti-miR-10b-5p and a 1-(3′,4′,5′-trimethoxyphenyl)-2-aryl-1 H -imidazole derivative is an encouraging strategy to boost the efficacy of anticancer therapies and at the same time to reduce side effects.
    Keywords microRNA ; anti-miR ; miR-10b-5p ; glioma ; apoptosis ; tubulin ; Biology (General) ; QH301-705.5 ; Chemistry ; QD1-999
    Subject code 570
    Language English
    Publishing date 2022-05-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  2. Article ; Online: Apoptosis Pathways Triggered by a Potent Antiproliferative Hybrid Chalcone on Human Melanoma Cells

    Irene Rodríguez / Ester Saavedra / Henoc del Rosario / Juan Perdomo / José Quintana / Filippo Prencipe / Paola Oliva / Romeo Romagnoli / Francisco Estévez

    International Journal of Molecular Sciences, Vol 22, Iss 13462, p

    2021  Volume 13462

    Abstract: The World Health Organization reported that approximately 324,000 new cases of melanoma skin cancer were diagnosed worldwide in 2020. The incidence of melanoma has been increasing over the past decades. Targeting apoptotic pathways is a potential ... ...

    Abstract The World Health Organization reported that approximately 324,000 new cases of melanoma skin cancer were diagnosed worldwide in 2020. The incidence of melanoma has been increasing over the past decades. Targeting apoptotic pathways is a potential therapeutic strategy in the transition to preclinical models and clinical trials. Some naturally occurring products and synthetic derivatives are apoptosis inducers and may represent a realistic option in the fight against the disease. Thus, chalcones have received considerable attention due to their potential cytotoxicity against cancer cells. We have previously reported a chalcone containing an indole and a pyridine heterocyclic rings and an α-bromoacryloylamido radical which displays potent antiproliferative activity against several tumor cell lines. In this study, we report that this chalcone is a potent apoptotic inducer for human melanoma cell lines SK-MEL-1 and MEL-HO. Cell death was associated with mitochondrial cytochrome c release and poly(ADP-ribose) polymerase cleavage and was prevented by a non-specific caspase inhibitor. Using SK-MEL-1 as a model, we found that the mechanism of cell death involves (i) the generation of reactive oxygen species, (ii) activation of the extrinsic and intrinsic apoptotic and mitogen-activated protein kinase pathways, (iii) upregulation of TRAIL, DR4 and DR5, (iv) downregulation of p21 Cip1/WAF1 and, inhibition of the NF-κB pathway.
    Keywords apoptosis ; caspases ; cytotoxicity ; hybrid chalcones ; extracellular signal-regulated kinases ; melanoma ; Biology (General) ; QH301-705.5 ; Chemistry ; QD1-999
    Subject code 610
    Language English
    Publishing date 2021-12-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  3. Article ; Online: Design, Synthesis and Biological Investigation of 2-Anilino Triazolopyrimidines as Tubulin Polymerization Inhibitors with Anticancer Activities

    Romeo Romagnoli / Paola Oliva / Filippo Prencipe / Stefano Manfredini / Federica Budassi / Andrea Brancale / Salvatore Ferla / Ernest Hamel / Diana Corallo / Sanja Aveic / Lorenzo Manfreda / Elena Mariotto / Roberta Bortolozzi / Giampietro Viola

    Pharmaceuticals, Vol 15, Iss 8, p

    2022  Volume 1031

    Abstract: A further investigation aiming to generate new potential antitumor agents led us to synthesize a new series of twenty-two compounds characterized by the presence of the 7-(3′,4′,5′-trimethoxyphenyl)-[1,2,4]triazolo[1,5- a ]pyrimidine pharmacophore ... ...

    Abstract A further investigation aiming to generate new potential antitumor agents led us to synthesize a new series of twenty-two compounds characterized by the presence of the 7-(3′,4′,5′-trimethoxyphenyl)-[1,2,4]triazolo[1,5- a ]pyrimidine pharmacophore modified at its 2-position. Among the synthesized compounds, three were significantly more active than the others. These bore the substituents p -toluidino ( 3d ), p -ethylanilino ( 3h ) and 3′,4′-dimethylanilino ( 3f ), and these compounds had IC 50 values of 30–43, 160–240 and 67–160 nM, respectively, on HeLa, A549 and HT-29 cancer cells. The p -toluidino derivative 3d was the most potent inhibitor of tubulin polymerization (IC 50 : 0.45 µM) and strongly inhibited the binding of colchicine to tubulin (72% inhibition), with antiproliferative activity superior to CA-4 against A549 and HeLa cancer cell lines. In vitro investigation showed that compound 3d was able to block treated cells in the G2/M phase of the cell cycle and to induce apoptosis following the intrinsic pathway, further confirmed by mitochondrial depolarization and caspase-9 activation. In vivo experiments conducted on the zebrafish model showed good activity of 3d in reducing the mass of a HeLa cell xenograft. These effects occurred at nontoxic concentrations to the animal, indicating that 3d merits further developmental studies.
    Keywords colchicine binding site ; antitumor activity ; [1,2,4]triazolo[1,5- a ]pyrimidine ; apoptosis ; microtubule-targeting agents ; Medicine ; R ; Pharmacy and materia medica ; RS1-441
    Language English
    Publishing date 2022-08-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  4. Article ; Online: Microfluidics and Electron Microscopy

    Luca Rima / Andri Fränkl / Anastasia Syntychaki / Paola Oliva / M. Zimmermann / Xavier Wildermuth / Rosemarie Sütterlin / Thomas Braun

    CHIMIA, Vol 74, Iss

    A Powerful Couple

    2020  Volume 11

    Keywords Cryo-em ; Microfluidics ; Nanoanalytics ; Single particle analysis ; Single-cell analysis ; Visual proteomics ; Chemistry ; QD1-999
    Language German
    Publishing date 2020-11-01T00:00:00Z
    Publisher Swiss Chemical Society
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  5. Article ; Online: Synthesis and Biological Evaluation of New Antitubulin Agents Containing 2-(3′,4′,5′-trimethoxyanilino)-3,6-disubstituted-4,5,6,7-tetrahydrothieno[2,3- c ]pyridine Scaffold

    Romeo Romagnoli / Filippo Prencipe / Paola Oliva / Barbara Cacciari / Jan Balzarini / Sandra Liekens / Ernest Hamel / Andrea Brancale / Salvatore Ferla / Stefano Manfredini / Matteo Zurlo / Alessia Finotti / Roberto Gambari

    Molecules, Vol 25, Iss 1690, p

    2020  Volume 1690

    Abstract: Two novel series of compounds based on the 4,5,6,7-tetrahydrothieno[2,3- c ]pyridine and 4,5,6,7-tetrahydrobenzo[ b ]thiophene molecular skeleton, characterized by the presence of a 3′,4′,5′-trimethoxyanilino moiety and a cyano or an alkoxycarbonyl group ...

    Abstract Two novel series of compounds based on the 4,5,6,7-tetrahydrothieno[2,3- c ]pyridine and 4,5,6,7-tetrahydrobenzo[ b ]thiophene molecular skeleton, characterized by the presence of a 3′,4′,5′-trimethoxyanilino moiety and a cyano or an alkoxycarbonyl group at its 2- or 3-position, respectively, were designed, synthesized, and evaluated for antiproliferative activity on a panel of cancer cell lines and for selected highly active compounds, inhibition of tubulin polymerization, and cell cycle effects. We have identified the 2-(3′,4′,5′-trimethoxyanilino)-3-cyano-6-methoxycarbonyl-4,5,6,7-tetrahydrothieno[2,3- c ]pyridine derivative 3a and its 6-ethoxycarbonyl homologue 3b as new antiproliferative agents that inhibit cancer cell growth with IC 50 values ranging from 1.1 to 4.7 μM against a panel of three cancer cell lines. Their interaction with tubulin at micromolar levels leads to the accumulation of cells in the G2/M phase of the cell cycle and to an apoptotic cell death. The cell apoptosis study found that compounds 3a and 3b were very effective in the induction of apoptosis in a dose-dependent manner. These two derivatives did not induce cell death in normal human peripheral blood mononuclear cells, suggesting that they may be selective against cancer cells. Molecular docking studies confirmed that the inhibitory activity of these molecules on tubulin polymerization derived from binding to the colchicine site.
    Keywords microtubules ; structure–activity relationship ; antiproliferative activity ; tubulin ; tetrahydrothieno[2,3- c ]pyridine ; Organic chemistry ; QD241-441
    Language English
    Publishing date 2020-04-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  6. Article ; Online: Synthesis and Biological Evaluation of 2-Substituted Benzyl-/Phenylethylamino-4-amino-5-aroylthiazoles as Apoptosis-Inducing Anticancer Agents

    Paola Oliva / Valentina Onnis / Elisa Balboni / Ernest Hamel / Francisco Estévez-Sarmiento / José Quintana / Francisco Estévez / Andrea Brancale / Salvatore Ferla / Stefano Manfredini / Romeo Romagnoli

    Molecules, Vol 25, Iss 2177, p

    2020  Volume 2177

    Abstract: Induction of apoptosis is a common chemotherapeutic mechanism to kill cancer cells The thiazole system has been reported over the past decades as a building block for the preparation of anticancer agents. A novel series of 2-arylalkylamino-4-amino-5-(3′, ... ...

    Abstract Induction of apoptosis is a common chemotherapeutic mechanism to kill cancer cells The thiazole system has been reported over the past decades as a building block for the preparation of anticancer agents. A novel series of 2-arylalkylamino-4-amino-5-(3′,4′,5′-trimethoxybenzoyl)-thiazole derivatives designed as dual inhibitors of tubulin and cyclin-dependent kinases (CDKs) were synthesized and evaluated for their antiproliferative activity in vitro against two cancer cell lines and, for selected highly active compounds, for interactions with tubulin and cyclin-dependent kinases and for cell cycle and apoptosis effects. Structure-activity relationships were elucidated for various substituents at the 2-position of the thiazole skeleton. Among the synthesized compounds, the most active analogues were found to be the p -chlorobenzylamino derivative 8e as well as the p -chloro and p -methoxyphenethylamino analogues 8f and 8k , respectively, which inhibited the growth of U-937 and SK-MEL-1 cancer cell lines with IC 50 values ranging from 5.7 to 12.2 μM. On U-937 cells, the tested compounds 8f and 8k induced apoptosis in a time and concentration dependent manner. These two latter molecules did not affect tubulin polymerization (IC 50 > 20 μM) nor CDK activity at a single concentration of 10 μM, suggesting alternative targets than tubulin and CDK for the compounds.
    Keywords microtubules ; structure-activity relationship ; antiproliferative activity ; pharmacophoric merging ; apoptosis ; Organic chemistry ; QD241-441
    Subject code 540
    Language English
    Publishing date 2020-05-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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