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http://dx.doi.org/10.13160/ricns.2014.7.4.241

Synthesis, Antibacterial, Docking and Anticancer Evaluation of N-Substituted Benzoyl Derivatives  

Arthi, P. (Post-Graduate and Research Department of Chemistry, The New College(Autonomous))
Shobana, S. (Department of Bioinformatics, School of Bioengineering, SRM University)
Srinivasan, P. (Department of Bioinformatics, Alagappa University)
Rahiman, A. Kalilur (Post-Graduate and Research Department of Chemistry, The New College(Autonomous))
Publication Information
Journal of Integrative Natural Science / v.7, no.4, 2014 , pp. 241-252 More about this Journal
Abstract
A series of N-benzoylated ligands incorporating three different benzoyl groups 2,2'-(benzoyliminodiethylene)-4-substituted phenols ($L^{1,4,7}$), 2,2'-(4-nitrobenzoyliminodiethylene)-4-substituted phenols ($L^{2,5,8}$) and 2,2'-(3,5-dinitrobenzoyliminodiethylene)-4-substituted phenols ($L^{3,6,9}$) were synthesized and characterized by IR, $^1H$ NMR, $^{13}C$ NMR and mass spectroscopy. The In vitro antibacterial activity of investigated ligands were tested against human pathogenic bacteria such as four Gram (-) Enterococcus faecalis, Pseudomonas aeruginosa, Staphylococcus aureus, Vibrio cholera, Vibrio harveyi and two Gram (+) Staphylococcus aureus, Streptococcus mutans. Furthermore, docking studies were undertaken to gain insight into the possible binding mode of these compounds with the binding site of the topoisomerase II (PDB: 4FM9) enzyme which is involved in DNA superhelicity and chromosome seggregation. The N-benzoylated derivatives $L^{5,7,8}$ have significant anticancer activity as Topoisomerase inhibitors. The ligands $L^5$ and $L^8$ were tested for their anticancer activity against human liver adenocarcinoma (HepG2) cell line with the MTT assay.
Keywords
Schiff-base Ligands; Antibacterial Activity; Docking Studies; Topoisomerase II; Cytotoxicity;
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