Investigation of selective cytotoxicity and determination of ligand induced apoptosis of a new acenaphtho [1,2-b] quinoxaline derivative.
Several new acenaphtho[1,2-b]quinoxaline derivatives were prepared by the reaction of o-phenylenediamines with acenaphthenequinones. The response of different carcinoid cell lines to these compounds were evaluated by MTT (3-(4,5-dimethylthiazol-2-yl)2,5-diphenyl tetrazolium bromide) assay and trypan blue exclusion tests. The cytotoxicity of 3,4-dinitroacenaphtho[1,2-b]quinoxaline (IIId) on the tested cell lines was confirmed by both tests. Furthermore, the MTT test showed a significant difference (p < 0.05) between the cytotoxicity of this compound on malignant cell lines of Caco-2, HT-29, T47D and non malignant mouse fibroblast cell line of NIH-3T3. An apoptosis inducing effect of compound IIId on K562 cells was detected by flow cytometry using Annexin-V-fluorescein isothiocyanate (AnV-FITC) and propidium iodide (PI) staining. The apoptosis induction (PI-/AnV+) in treated K562 cells was significantly (p < 0.01) more at 0.5 microg/ml concentration of compound IIId in comparison to all other concentrations of this compound and also doxorubicin (CAS 25316-40-9) (250 nM).
Mahjoob
Elham
E
Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran.
Khalaj
Ali
A
Ostad
Seyed Nasser
SN
Azizi
Ebrahim
E
Fouladdel
Shamileh
S
Tavajohi
Shohreh
S
Salehi
Raha
R
Dowlatabadi
Reza
R
D016475:3T3 Cells; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D018938:Caco-2 Cells; D005434:Flow Cytometry; D019073:HT29 Cells; D006801:Humans; D007202:Indicators and Reagents; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D011810:Quinoxalines / Q000138:chemical synthesis / Q000494:pharmacology; D013055:Spectrophotometry, Infrared
D000970:Antineoplastic Agents; D007202:Indicators and Reagents; D008024:Ligands; D011810:Quinoxalines