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Synthesis and biological evaluation of novel 3-benzylcoumarin-imidazolium salts
Affiliation:1. Research Laboratory of Environmental Sciences and Technologies (LR16ES09), Higher Institute of Environmental Sciences and Technology, University of Carthage, Hammam-Lif, Tunisia;2. Laboratory of Microorganisms and Biomolecules of the Center of Biotechnology of Sfax-Tunisia. Road of Sidi Mansour, Km 6 B.P. 1117, 3018 Sfax, Tunisia;3. Zoology Department, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia;4. İnönü University, Faculty of Science and Art, Department of Chemistry, Malatya, Turkey;5. Chemistry Department, College of Science and Arts, Qassim University, Al-Rass, Saudi Arabia;1. Department of Macromolecular Physics, Faculty of Physics, Adam Mickiewicz University, Umultowska 85, 61-614 Poznaſ, Poland;2. Joint SAXS Laboratory, Faculty of Physics, Adam Mickiewicz University, Umultowska 85, 61-614 Poznaſ, Poland;1. Department of Chemistry, College of Science, University of Kufa, Najaf, Iraq;2. The School of Chemical Sciences, Universiti Sains Malaysia, 11800 USM, Penang, Malaysia;3. Centre for Nano and Material Sciences, Jain University, Jain Global Campus, Kanakapura, Ramanagaram, Bangalore 562112, India;4. EMAN Research and Testing Laboratory, The School of Pharmaceutical Sciences, Universiti Sains Malaysia, 11800 USM, Penang, Malaysia;1. The University of Sydney, Faculty of Pharmacy, NSW, 2006, Sydney, Australia;2. Erciyes University, Faculty of Sciences, Department of Chemistry, Talas Street, 38039, Kayseri, Turkey;3. Inönü University, Faculty of Arts and Sciences, Department of Chemistry, 44280, Malatya, Turkey
Abstract:A series of novel 3-benzylcoumarin-imidazolium salts were prepared and evaluated in vitro against a panel of human tumor cell lines. The results showed that the existence of 5,6-dimethyl-benzimidazole ring and substitution of the imidazolyl-3-position with a naphthylacyl group were vital for modulating cytotoxic activity. Notably, compound 38 was found to be the most potent derivative with IC50 values of 2.04–4.51 μM against five human tumor cell lines, while compound 34 were more selective to SW-480 cell lines with IC50 value 40.0-fold lower than DDP. Mechanism of action studies indicated that compound 38 can cause the G0/G1 phase cell cycle arrest and apoptosis in SMMC-7721 cell lines.
Keywords:3-Benzylcoumarin  Imidazolium salts  Biological evaluation  Cytotoxic activity  Structure-activity relationships
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