In Vitro Antiplasmodial Activity and Cytotoxic Effect of (Z)-2-Benzylidene-4, 6-Dimethoxybenzofuran-3(2H)-One Derivatives

  • Ali RAMAZANI Dept. of Biotechnology, School of Pharmacy, Zanjan University of Medical Sciences, Zanjan, Iran
  • Reza HAMIDNEZHAD Dept. of Biotechnology, School of Pharmacy, Zanjan University of Medical Sciences, Zanjan, Iran
  • Alireza FOROUMADI Dept. of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran
  • Seyed Abbas MIRZAEI Dept. of Biotechnology, School of Pharmacy, Zanjan University of Medical Sciences, Zanjan, Iran
  • Somayyeh MADDAHI Iranian Blood Transfusion Organization, Zanjan, Iran
  • Seyed Mehdi HASSANZADEH BCG Vaccine Unit, Pasteur Institute of Iran, Tehran, Iran
Keywords: Plasmodium falciparum, Aurones, Cytotoxicity

Abstract

Background: Aurones are naturally occurring compounds that belong to flavenoids family and have antiplasmodial effects. This study investigated some new aurones derivatives against chloroquine sensitive Plasmodium falciparum. Here we report the synthesis, in vitro antiplasmodial activity and cytotoxic evaluation of 11 compound from derivatives of (Z)-2- benzylidene-4, 6-dimethoxybenzofuran-3(2H)-one.Methods: The cytotoxic evaluations of active compounds were performed with MTT (3-[4, 5-dimethylthiazol-2-yl]-2, 5 diphenyltetrazolium bromide) assay on human breast cancer cell lines; MCF7 and T47D.Results: From 11 compounds M3, M6 and M7 compounds showed good antiplasmodial effect against chloroquine-sensitive 3D strain of P. falciparum with IC50 (50% inhibitory concentration) values of 7.82, 7.27 and 2.3 µM respectively. No noticeable toxicity was‌ observed with these compounds when tested against tested cell lines. Conclusion: The replacement of the 4 and 5 positions at ring B of aurone derivatives, with propoxy and bromide (Br) respectively was revealed highly advantageous for their antiplasmodial effect.

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Published
2016-12-21
How to Cite
1.
RAMAZANI A, HAMIDNEZHAD R, FOROUMADI A, MIRZAEI SA, MADDAHI S, HASSANZADEH SM. In Vitro Antiplasmodial Activity and Cytotoxic Effect of (Z)-2-Benzylidene-4, 6-Dimethoxybenzofuran-3(2H)-One Derivatives. IJPA. 11(3):371-6.
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Short Communication(s)