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| Verfasst von: | Wenzel, Nicole [VerfasserIn]  |
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| | Chavain, Natascha [VerfasserIn] |
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| | Wang, Yulin [VerfasserIn] |
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| | Friebolin, Wolfgang [VerfasserIn] |
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| | Maes, Louis [VerfasserIn] |
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| | Pradines, Bruno [VerfasserIn] |
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| | Lanzer, Michael [VerfasserIn] |
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| | Yardley, Vanessa [VerfasserIn] |
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| | Brun, Reto [VerfasserIn] |
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| | Herold-Mende, Christel [VerfasserIn] |
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| | Biot, Christophe [VerfasserIn] |
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| | Tóth, Katalin [VerfasserIn] |
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| | Davioud-Charvet, Elisabeth [VerfasserIn] |
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| Titel: | Antimalarial versus cytotoxic properties of dual drugs derived from 4-aminoquinolines and Mannich bases |
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| Titelzusatz: | Interaction with DNA |
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| Verf.angabe: | Nicole I. Wenzel, Natascha Chavain, Yulin Wang, Wolfgang Friebolin, Louis Maes, Bruno Pradines, Michael Lanzer, Vanessa Yardley, Reto Brun, Christel Herold-Mende, Christophe Biot, Katalin Tóth, and Elisabeth Davioud-Charvet |
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| E-Jahr: | 2010 |
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| Jahr: | 22 April 2010 |
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| Umfang: | 13 S. |
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| Illustrationen: | Diagramme |
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| Fussnoten: | Gesehen am 16.11.2023 |
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| Titel Quelle: | Enthalten in: Journal of medicinal chemistry |
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| Ort Quelle: | Washington, DC : ACS, 1959 |
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| Jahr Quelle: | 2010 |
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| Band/Heft Quelle: | 53(2010), 8 vom: Apr., Seite 3214-3226 |
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| ISSN Quelle: | 1520-4804 |
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| Abstract: | The synthesis and biological evaluation of new organic and organometallic dual drugs designed as potential antimalarial agents are reported. A series of 4-aminoquinoline-based Mannich bases with variations in the aliphatic amino side chain were prepared via a three-steps synthesis. These compounds were also tested against chloroquine-susceptible and chloroquine-resistant strains of Plasmodium falciparum and assayed for their ability to inhibit the formation of β-hematin in vitro using a colorimetric β-hematin inhibition assay. Several compounds showed a marked antimalarial activity, with IC50 and IC90 values in the low nM range but also a high cytotoxicity against mammalian cells, in particular a highly drug-resistant glioblastoma cell line. The newly designed compounds revealed high DNA binding properties, especially for the GC-rich domains. Altogether, these dual drugs seem to be more appropriate to be developed as antiproliferative agents against mammalian cancer cells than Plasmodium parasites. |
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| DOI: | doi:10.1021/jm9018383 |
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| URL: | Bitte beachten Sie: Dies ist ein Bibliographieeintrag. Ein Volltextzugriff für Mitglieder der Universität besteht hier nur, falls für die entsprechende Zeitschrift/den entsprechenden Sammelband ein Abonnement besteht oder es sich um einen OpenAccess-Titel handelt.
Volltext: https://doi.org/10.1021/jm9018383 |
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| | DOI: https://doi.org/10.1021/jm9018383 |
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| Datenträger: | Online-Ressource |
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| Sprache: | eng |
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| K10plus-PPN: | 1870489896 |
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| Verknüpfungen: | → Zeitschrift |
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Antimalarial versus cytotoxic properties of dual drugs derived from 4-aminoquinolines and Mannich bases / Wenzel, Nicole [VerfasserIn]; 22 April 2010 (Online-Ressource)
