1229445-13-9Relevant academic research and scientific papers
Biologically active carbazole derivatives: Focus on oxazinocarbazoles and related compounds
Bouaziz, Zouhair,Issa, Samar,Gentili, Jacques,Gratz, Andreas,Bollacke, Andre,Kassack, Matthias,Jose, Joachim,Herfindal, Lars,Gausdal, Gro,Doskeland, Stein Ove,Mullié, Catherine,Sonnet, Pascal,Desgrouas, Camille,Taudon, Nicolas,Valdameri, Glaucio,Di Pietro, Attilio,Baitiche, Milad,Le Borgne, Marc
, p. 180 - 188 (2015/04/14)
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 14.0μM, respectively. Further chemical syntheses were realized and the 7-isopropyl oxazinocarbazole derivative 2 displayed a stronger activity against CK2 (IC50=1.40μM). 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 62μM. Further investigations were also reported on antibacterial and antiplasmodial activities. No significant inhibitory activity on ABCG2 efflux pump was detected.
Synthesis and antiproliferative activity of oxazinocarbazole and N,N-bis(carbazolylmethyl)amine derivatives
Issa, Samar,Walchshofer, Nadia,Kassab, Issam,Termoss, Hussein,Chamat, Soulaima,Geahchan, Aziz,Bouaziz, Zouhair
experimental part, p. 2567 - 2577 (2010/07/09)
The synthesis, structure elucidation and antitumoral activity of novel heterocyclic compounds containing a carbazole nucleus are reported. Oxazinocarbazoles were synthesized by application of the Mannich reaction to the corresponding hydroxylated derivatives leading to 41 new molecules. Their cytotoxic activity was evaluated against various human tumor cell lines including three leukemic cell lines: CEM and Jurkat (type T), Raji (type B); breast cancer cell line (MCF-7); colorectal cancer cell line (Caco-2). A primary screening at 100 μM allowed the selection of the 10 most active compounds, which showed an antiproliferative activity on all the cell lines. A dose-effect study between 12.5 and 100 μM sorted two compounds with a significant activity: 5t and 7e against leukemic cell lines CEM, Jurkat and Raji with IC50 values around 12 μM.
