IN VITRO CYTOTOXICITY EVALUATION OF SIXTEEN NEW N-PIPERAZINYL QUINOLONE DERIVATIVES AGAINST A PANEL OF TUMOR CELL LINES

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RAJABALIAN SAEID; FOROUMADI A.R.; HEIDARI M.R.; KARIMZADEH R.; PARDAKHTI A.; HOSSEIN RAFAT

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Journal: Journal of Kerman University of Medical Sciences Year:2007 | Volume:14 | Issue:2 Page(s): 100-108

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Title

IN VITRO CYTOTOXICITY EVALUATION OF SIXTEEN NEW N-PIPERAZINYL QUINOLONE DERIVATIVES AGAINST A PANEL OF TUMOR CELL LINES

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Keywords

CYTOTOXICITYQ2

FLUOROQUINOLONEQ3

MTT- ASSAYQ2

ETOPOSIDEQ3

Abstract

Introduction: FLUOROQUINOLONEs are potent inhibitors of bacterial topoisomerase II. They can also inhibit eukaryotic topoisomerase, and may confer antitumoral properties. Method: In this study the antitumoral activity of a new series of N-substituted piperazinyl- FLUOROQUINOLONEs against a panel of human tumor cell lines was determined by MTT assays. Results: Among the tested compounds N-[2- (5-bromo-2-thienyl)-2-oxoethyl ] (C1,N1,E1), N-[ 2- (5-bromo-2-thienyl)-2-(hydroxyimino) ethyl]( C2,N2,E2) and N-[2-(5-bromo-2-thienyl)-2-(phenylmethoxyimino) ethyl] (C3, N3, E3) piperazinyl quinolones exhibited the most cytotoxic activities (mean IC50s = 2.5 to 3 mg/ml), comparable to that of the ETOPOSIDE (mean IC50= 1.7mg/ml). Replacement of the 5- bromo-2-thienyl with 4- fluorophenyl or 2,6- difluorophenyl rings leads to variable inhibition activity. The quinolone activity was enhanced by the presence of chlorine and two fluorine atoms at the benzyl and phenyl groups, especially against ACHN renal adenocarcinoma cell line. Conclusion: These data suggest that these series of quinolones provide good models for the further design of potent antitumor compounds.

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APA: Copy

RAJABALIAN, SAEID, FOROUMADI, A.R., HEIDARI, M.R., KARIMZADEH, R., PARDAKHTI, A., & HOSSEIN, RAFAT. (2007). IN VITRO CYTOTOXICITY EVALUATION OF SIXTEEN NEW N-PIPERAZINYL QUINOLONE DERIVATIVES AGAINST A PANEL OF TUMOR CELL LINES. JOURNAL OF KERMAN UNIVERSITY OF MEDICAL SCIENCES, 14(2), 100-108. SID. https://sid.ir/paper/451/en

Vancouver: Copy

RAJABALIAN SAEID, FOROUMADI A.R., HEIDARI M.R., KARIMZADEH R., PARDAKHTI A., HOSSEIN RAFAT. IN VITRO CYTOTOXICITY EVALUATION OF SIXTEEN NEW N-PIPERAZINYL QUINOLONE DERIVATIVES AGAINST A PANEL OF TUMOR CELL LINES. JOURNAL OF KERMAN UNIVERSITY OF MEDICAL SCIENCES[Internet]. 2007;14(2):100-108. Available from: https://sid.ir/paper/451/en

IEEE: Copy

SAEID RAJABALIAN, A.R. FOROUMADI, M.R. HEIDARI, R. KARIMZADEH, A. PARDAKHTI, and RAFAT HOSSEIN, “IN VITRO CYTOTOXICITY EVALUATION OF SIXTEEN NEW N-PIPERAZINYL QUINOLONE DERIVATIVES AGAINST A PANEL OF TUMOR CELL LINES,” JOURNAL OF KERMAN UNIVERSITY OF MEDICAL SCIENCES, vol. 14, no. 2, pp. 100–108, 2007, [Online]. Available: https://sid.ir/paper/451/en

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