원문정보
초록
영어
A series of N-benzoylated ligands incorporating three different benzoyl groups 2,2’-(benzoyliminodiethylene)- 4- substituted phenols (L1,4,7), 2,2’-(4-nitrobenzoyliminodiethylene)-4-substituted phenols (L2,5,8) and 2,2’-(3,5- dinitrobenzoyliminodiethylene)-4-substituted phenols (L3,6,9) were synthesized and characterized by IR, 1H NMR, 13C 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 Nbenzoylated derivatives L5, 7, 8 have significant anticancer activity as Topoisomerase inhibitors. The ligands L5 and L8 were tested for their anticancer activity against human liver adenocarcinoma (HepG2) cell line with the MTT assay.
목차
1. Introduction
2. Experimental Section
2.1. Synthesis
2.2. Synthesis of Ligands
2.3. In Vitro Antibacterial Screening
2.4. Molecular Docking Studies
2.5. Cell Proliferation Assay
3. Results and Discussion
3.1. In vitro Antibacterial Screening
3.2. Molecular Docking Studies
3.3. Admet Results
3.4. Cytotoxicity Evaluation
4. Conclusions
Acknowledgements
References