Quinoline-Based p300 Histone Acetyltransferase Inhibitors with Pro-apoptotic Activity in Human Leukemia U937 Cells
| Autor: | Rosaria Benedetti, Simone Carradori, Gianluca Sbardella, Alessia Lenoci, Stefano Tomassi, Lucia Altucci, Ettore Novellino, Veronica Rodriguez, Antonello Mai, Patrizia Filetici, Daniela Secci, Sabrina Castellano, Mariarosaria Conte, Dante Rotili |
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| Přispěvatelé: | Lenoci, A, Tomassi, S, Conte, M, Benedetti, R, Rodriguez, V, Carradori, S, Secci, D, Castellano, S, Sbardella, G, Filetici, P, Novellino, E, Altucci, Lucia, Rotili, D, Mai, A., Alessia, Lenoci, Tomassi, Stefano, Mariarosaria, Conte, Rosaria, Benedetti, Veronica, Rodriguez, Simone, Carradori, Daniela, Secci, Sabrina, Castellano, Gianluca, Sbardella, Patrizia, Filetici, Novellino, Ettore, Lucia, Altucci, Dante, Rotili, Antonello, Mai |
| Jazyk: | angličtina |
| Rok vydání: | 2014 |
| Předmět: |
Biochemistry
chemistry.chemical_compound 0302 clinical medicine lysine acetyltransferases (KATs) quinoline Drug Discovery Tumor Cells Cultured Enzyme Inhibitors General Pharmacology Toxicology and Pharmaceutics 0303 health sciences Molecular Structure biology U937 cell Quinoline apoptosis leukemia Cell Differentiation U937 Cells 3. Good health Leukemia 030220 oncology & carcinogenesis Quinolines Molecular Medicine epigenetic U937 Antineoplastic Agents p300 Structure-Activity Relationship 03 medical and health sciences Histone H3 HATs histone acetyltransferase inhibitors medicine Humans cancer Epigenetics epigenetics HAT structure–activity relationships 030304 developmental biology Pharmacology Dose-Response Relationship Drug structure-activity relationships Organic Chemistry Histone acetyltransferase medicine.disease Molecular biology chemistry Apoptosis Acetylation biology.protein Drug Screening Assays Antitumor |
| Zdroj: | ChemMedChem; Vol 9 ChemMedChem 9 (2014): 542–548. doi:10.1002/cmdc.201300536 info:cnr-pdr/source/autori:Lenoci, Alessia; Tomassi, Stefano; Conte, Mariarosaria; Benedetti, Rosaria; Rodriguez, Veronica; Carradori, Simone; Secci, Daniela; Castellano, Sabrina; Sbardella, Gianluca; Filetici, Patrizia; Novellino, Ettore; Altucci, Lucia; Rotili, Dante; Mai, Antonello/titolo:Quinoline-Based p300 Histone Acetyltransferase Inhibitors with Pro-apoptotic Activity in Human Leukemia U937 Cells/doi:10.1002%2Fcmdc.201300536/rivista:ChemMedChem (Print)/anno:2014/pagina_da:542/pagina_a:548/intervallo_pagine:542–548/volume:9 |
| DOI: | 10.1002/cmdc.201300536 |
| Popis: | Chemical manipulations performed on 2-methyl-3-carbethoxyquinoline (1), a histone acetyltransferase inhibitor previously identified by our research group and active at the sub-millimolar/millimolar level, led to compounds bearing higher alkyl groups at the C2-quinoline or additional side chains at the C6-quinoline positions. Such compounds displayed at least threefold improved inhibitory potency toward p300 protein lysine acetyltransferase activity; some of them decreased histone H3 and H4 acetylation levels in U937 cells and induced high degrees of apoptosis (three compounds >10-fold higher than compound 1) after treatment of U937 cells. |
| Databáze: | OpenAIRE |
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