Biologically active carbazole derivatives: focus on oxazinocarbazoles and related compounds
| Autor: | Zouhair Bouaziz, Gro Gausdal, Pascal Sonnet, Andre Bollacke, Joachim Jose, Attilio Di Pietro, Matthias U. Kassack, Catherine Mullié, Samar Issa, Andreas Gratz, Stein Ove Døskeland, Jacques Gentili, Camille Desgrouas, Lars Herfindal, Glaucio Valdameri, Marc Le Borgne, Milad Baitiche, Nicolas Taudon |
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| Přispěvatelé: | Molécules bioactives et chimie médicinale (B2MC), Université Claude Bernard Lyon 1 (UCBL), Université de Lyon-Université de Lyon, Laboratoire EBInnov, Ecole de Biologie Industrielle, Institut für Pharmazeutische und Medizinische Chemie, Westfälische Wilhelms-Universität Münster = University of Münster (WWU), University of Bergen (UiB), Laboratoire de Glycochimie, des Antimicrobiens et des Agro-ressources - UMR CNRS 7378 (LG2A ), Université de Picardie Jules Verne (UPJV)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Infections Parasitaires : Transmission, Physiopathologie et Thérapeutiques (IP-TPT), Institut de Recherche pour le Développement (IRD)-Aix Marseille Université (AMU)-Assistance Publique - Hôpitaux de Marseille (APHM)-Service de Santé des Armées, Bases moléculaires et structurales des systèmes infectieux (BMSSI), Université de Lyon-Université de Lyon-Centre National de la Recherche Scientifique (CNRS), Westfälische Wilhelms-Universität Münster (WWU), Institut de Chimie du CNRS (INC)-Université de Picardie Jules Verne (UPJV)-Centre National de la Recherche Scientifique (CNRS) |
| Jazyk: | angličtina |
| Rok vydání: | 2015 |
| Předmět: |
Cell Survival
Stereochemistry Plasmodium falciparum Carbazoles Antineoplastic Agents [SDV.CAN]Life Sciences [q-bio]/Cancer Microbial Sensitivity Tests [CHIM.THER]Chemical Sciences/Medicinal Chemistry [SDV.BC]Life Sciences [q-bio]/Cellular Biology Gram-Positive Bacteria 010402 general chemistry 01 natural sciences Chemical synthesis Antimalarials chemistry.chemical_compound Parasitic Sensitivity Tests Cell Line Tumor Gram-Negative Bacteria Oxazines Drug Discovery medicine Humans Cytotoxicity Protein Kinase Inhibitors Protein Kinase C ComputingMilieux_MISCELLANEOUS Pharmacology Mitoxantrone Molecular Structure biology 010405 organic chemistry Chemistry Carbazole Biological activity General Medicine [SDV.SP]Life Sciences [q-bio]/Pharmaceutical sciences medicine.disease biology.organism_classification [SDV.MP.BAC]Life Sciences [q-bio]/Microbiology and Parasitology/Bacteriology Anti-Bacterial Agents 0104 chemical sciences 3. Good health Leukemia Cell culture medicine.drug |
| Zdroj: | Journal of Enzyme Inhibition and Medicinal Chemistry Journal of Enzyme Inhibition and Medicinal Chemistry, 2015, 30 (2), pp.180-188. ⟨10.3109/14756366.2014.899594⟩ Journal of Enzyme Inhibition and Medicinal Chemistry, Informa Healthcare, 2015, 30 (2), pp.180-188. ⟨10.3109/14756366.2014.899594⟩ |
| ISSN: | 1475-6366 1475-6374 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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