In Vitro Cytotoxicity Evaluation of Sixteen New N-Piperazinyl Quinolone Derivatives Against A Panel Of Tumor Cell Lines
سال انتشار: 1386
نوع سند: مقاله ژورنالی
زبان: فارسی
مشاهده: 80
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شناسه ملی سند علمی:
JR_JKMU-14-4_003
تاریخ نمایه سازی: 14 اسفند 1402
چکیده مقاله:
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 piperazinylfluoroquinolones against a panel of human tumor cell lines was determined by MTT assays. Results: Among the tested compounds N-[۲- (۵-bromo-۲-thienyl)-۲-oxoethyl ] (C۱,N۱,E۱), N-[ ۲- (۵-bromo-۲-thienyl)-۲-(hydroxyimino) ethyl]( C۲,N۲,E۲) and N-[۲-(۵-bromo-۲-thienyl)-۲- (phenylmethoxyimino) ethyl] (C۳,N۳,E۳) piperazinyl quinolones exhibited the most cytotoxic activities (mean IC۵۰s = ۲.۵ to ۳ µg/ml), comparable to that of the Etoposide (mean IC۵۰= ۱.۷µg/ml). Replacement of the ۵- bromo-۲-thienyl with ۴- fluorophenyl or ۲,۶- difluorophenyl rings leads to variable inhibition activity. The quinolone activity was enhanced by the presence of a 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.
کلیدواژه ها:
نویسندگان
S Rajabalian
Researcher, Kerman Neuroscience Research Center, Kerman University of Medical Sciences, Kerman, Iran
A.R Foroumadi
Associate Professor of Pharmaceutics, School of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
M.R Heidari
Professor of Pharmacology, School of Pharmacy, Kerman University of Medical Sciences, Kerman, Iran
R Karimzadeh
Pharmacist
A Pardakhti
Assistant Professor of Pharmacology, School of Pharmacy and Pharmaceutical Technology Research Center, Kerman University of Medical Sciences, Kerman, Iran
R Hosseini
Researcher, Kerman Neuroscience Research Center, Kerman University of Medical Sciences, Kerman, Iran