Search

Your search keyword '"Lenoci, Alessia"' showing total 12 results
Start Over Author "Lenoci, Alessia"
12 results on '"Lenoci, Alessia"'

5. A novel orally active water-soluble inhibitor of human glutathione transferase exerts a potent and selective antitumor activity against human melanoma xenografts

Author

De Luca, Anastasia, primary, Rotili, Dante, additional, Carpanese, Debora, additional, Lenoci, Alessia, additional, Calderan, Laura, additional, Scimeca, Manuel, additional, Mai, Antonello, additional, Bonanno, Elena, additional, Rosato, Antonio, additional, Geroni, Cristina, additional, Quintieri, Luigi, additional, and Caccuri, Anna Maria, additional

Published
2015
Full Text
View/download PDF

6. 1,3,4-Oxadiazole-Containing Histone Deacetylase Inhibitors: Anticancer Activities in Cancer Cells

Author

Valente, Sergio, primary, Trisciuoglio, Daniela, additional, De Luca, Teresa, additional, Nebbioso, Angela, additional, Labella, Donatella, additional, Lenoci, Alessia, additional, Bigogno, Chiara, additional, Dondio, Giulio, additional, Miceli, Marco, additional, Brosch, Gerald, additional, Del Bufalo, Donatella, additional, Altucci, Lucia, additional, and Mai, Antonello, additional

Published
2014
Full Text
View/download PDF

7. Discovery of salermide-related sirtuin inhibitors: Binding mode studies and antiproliferative effects in cancer cells including cancer stem cells

Author

Rotili, Dante, Tarantino, Domenico, Nebbioso, Angela, Paolini, Chantal, Huidobro, Covadonga, Lara, Ester, Mellini, Paolo, Lenoci, Alessia, Pezzi, Riccardo, Botta, Giorgia, Lahtela-Kakkonen, Maija, Poso, Antti, Steinkühler, Christian, Gallinari, Paola, De Maria Marchiano, Ruggero, Fraga, Mario, Esteller, Manel, Altucci, Lucia, Mai, Antonello, De Maria Marchiano, Ruggero (ORCID:0000-0003-2255-0583), Rotili, Dante, Tarantino, Domenico, Nebbioso, Angela, Paolini, Chantal, Huidobro, Covadonga, Lara, Ester, Mellini, Paolo, Lenoci, Alessia, Pezzi, Riccardo, Botta, Giorgia, Lahtela-Kakkonen, Maija, Poso, Antti, Steinkühler, Christian, Gallinari, Paola, De Maria Marchiano, Ruggero, Fraga, Mario, Esteller, Manel, Altucci, Lucia, Mai, Antonello, and De Maria Marchiano, Ruggero (ORCID:0000-0003-2255-0583)

Abstract

Chemical changes performed on 1a (sirtinol) led to a series of SIRT1/2 inhibitors, in some cases more potent than 1a mainly against SIRT1. Tested in human leukemia U937 cells, the benzamide and anilide derivatives 1b, 1c, 2b, and 2c as well as the 4-(2-phenylpropyl)thioanalogue 4c showed huge apoptosis induction, while some sulfinyl and sulfonyl derivatives (5b, 5c, and 6a-c) were highly efficient in granulocytic differentiation. When assayed in human leukemia MOLT4 as well as in human breast MDA-MB-231 and colon RKO cancer cell lines, the anilide 2b (salermide) and the phenylpropylthio analogue 4b emerged as the most potent antiproliferative agents. Tested on colorectal carcinoma and glioblastoma multiforme cancer stem cells (CSCs) from patients, 2b was particularly potent against colorectal carcinoma CSCs, while 4b, 6a, and the SIRT2-selective inhibitor AGK-2 showed the highest effect against glioblastoma multiforme CSCs. Such compounds will be further explored for their broad-spectrum anticancer properties. © 2012 American Chemical Society.

Published
2012

8. Quinoline‐Based p300 Histone Acetyltransferase Inhibitors with Pro‐apoptotic Activity in Human Leukemia U937 Cells

Author

Lenoci, Alessia, primary, Tomassi, Stefano, additional, Conte, Mariarosaria, additional, Benedetti, Rosaria, additional, Rodriguez, Veronica, additional, Carradori, Simone, additional, Secci, Daniela, additional, Castellano, Sabrina, additional, Sbardella, Gianluca, additional, Filetici, Patrizia, additional, Novellino, Ettore, additional, Altucci, Lucia, additional, Rotili, Dante, additional, and Mai, Antonello, additional

Published
2014
Full Text
View/download PDF

9. Nitrobenzoxadiazole-based GSTP1-1 inhibitors containing the full peptidyl moiety of (pseudo)glutathione.

Author

Luisi, Grazia, Mollica, Adriano, Carradori, Simone, Lenoci, Alessia, De Luca, Anastasia, and Caccuri, Anna Maria

Subjects
NITROBENZOIC acid, GLUTATHIONE transferase, ENZYME inhibitors, DRUG resistance, ONCOLOGY, PEPTIDE drugs, FUNCTIONAL groups
Abstract

Context: The inhibition of glutathioneS-transferase P1-1 (GSTP1-1) is a sound strategy to overcome drug resistance in oncology practice. Objective: The nitrobenzoxadiazolyl (NBD)S-conjugate of glutathione and the corresponding γ-oxa-glutamyl isostere (compounds1and5, respectively) have been disclosed as GST inhibitors. The rationale of their design is discussed in juxtaposition to non-peptide NBD thioethers. Materials and methods: Synthesis of derivatives1and5andin vitroevaluation on human GSTP1-1 and M2-2 are reported. Results: Conjugates1and5were found to be low micromolar inhibitors of both isoforms. Furthermore, they display a threefold reduction in selectivity for GSTM2-2 over the P1-1 isozyme in comparison with the potent non-peptide inhibitor nitrobenzoxadiazolyl-thiohexanol (NBDHEX). Discussion and conclusions: Spectroscopic data are congruent with the formation of a stable sigma-complex between GSH and the inhibitors in the protein active site. Conjugate5is suitable forin vivomodulation of GST activity in cancer treatment. [ABSTRACT FROM PUBLISHER]

Published
2016
Full Text
View/download PDF

10. Discovery of Salermide-Related Sirtuin Inhibitors: Binding Mode Studies and Antiproliferative Effects in Cancer Cells Including Cancer Stem Cells

Author

Rotili, Dante, primary, Tarantino, Domenico, additional, Nebbioso, Angela, additional, Paolini, Chantal, additional, Huidobro, Covadonga, additional, Lara, Ester, additional, Mellini, Paolo, additional, Lenoci, Alessia, additional, Pezzi, Riccardo, additional, Botta, Giorgia, additional, Lahtela-Kakkonen, Maija, additional, Poso, Antti, additional, Steinkühler, Christian, additional, Gallinari, Paola, additional, De Maria, Ruggero, additional, Fraga, Mario, additional, Esteller, Manel, additional, Altucci, Lucia, additional, and Mai, Antonello, additional

Published
2012
Full Text
View/download PDF

12. Discovery of Salermide-RelatedSirtuin Inhibitors:Binding Mode Studies and Antiproliferative Effects in Cancer CellsIncluding Cancer Stem Cells.

Author

Rotili, Dante, Tarantino, Domenico, Nebbioso, Angela, Paolini, Chantal, Huidobro, Covadonga, Lara, Ester, Mellini, Paolo, Lenoci, Alessia, Pezzi, Riccardo, Botta, Giorgia, Lahtela-Kakkonen, Maija, Poso, Antti, Steinkühler, Christian, Gallinari, Paola, De Maria, Ruggero, Fraga, Mario, Esteller, Manel, Altucci, Lucia, and Mai, Antonello

Published
2012
Full Text
View/download PDF

Catalog

Books, media, physical & digital resources
See catalog results