학술논문
Biologically active carbazole derivatives: focus on oxazinocarbazoles and related compounds.
Document Type
Article
Author
Bouaziz, Zouhair; Issa, Samar; Gentili, Jacques; Gratz, Andreas; Bollacke, Andre; Kassack, Matthias; Jose, Joachim; Herfindal, Lars; Gausdal, Gro; Døskeland, Stein Ove; Mullié, Catherine; Sonnet, Pascal; Desgrouas, Camille; Taudon, Nicolas; Valdameri, Glaucio; Di Pietro, Attilio; Baitiche, Milad; Le Borgne, Marc
Source
Subject
*BIOACTIVE compounds
*CARBAZOLE derivatives
*QUINONE
*CELL-mediated cytotoxicity
*CHEMICAL synthesis
*ANTIBACTERIAL agents
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Language
ISSN
1475-6366
Abstract
Four series of carbazole derivatives, including N-substituted-hydroxycarbazoles, oxazinocarbazoles, isoxazolocarbazolequinones, and pyridocarbazolequinones, were studied using diverse biological test methods such as a CE-based assay for CK2 activity measurement, a cytotoxicity assay with IPC-81 cell line, determination of MIC of carbazole derivatives as antibacterial agents, a Plasmodium falciparum susceptibility assay, and an ABCG2-mediated mitoxantrone assay. Two oxazinocarbazoles Ib and Ig showed CK2 inhibition with IC50 = 8.7 and 14.0 µM, respectively. Further chemical syntheses were realized and the 7-isopropyl oxazinocarbazole derivative 2 displayed a stronger activity against CK2 (IC50 = 1.40 µM). Oxazinocarbazoles Ib, Ig, and 2 were then tested against IPC-81 leukemia cells and showed the ability to induce leukemia cell death with IC50 values between 57 and 62 μM. Further investigations were also reported on antibacterial and antiplasmodial activities. No significant inhibitory activity on ABCG2 efflux pump was detected. [ABSTRACT FROM AUTHOR]