1. Benzimidazole - Schiff bases and their complexes: synthesis, anticancer activity and molecular modeling as Aurora kinase inhibitor.
- Author
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Magd-El-Din AA, Mousa HA, Labib AA, Hassan AS, Abd El-All AS, Ali MM, El-Rashedy AA, and El-Desoky AH
- Subjects
- Animals, Antineoplastic Agents pharmacology, Antineoplastic Agents therapeutic use, Aurora Kinases metabolism, Benzimidazoles pharmacology, Benzimidazoles therapeutic use, Carcinoma, Ehrlich Tumor drug therapy, Hep G2 Cells, Humans, MCF-7 Cells, Male, Mice, Molecular Docking Simulation, Protein Kinase Inhibitors pharmacology, Protein Kinase Inhibitors therapeutic use, Schiff Bases chemistry, Antineoplastic Agents chemical synthesis, Aurora Kinases antagonists & inhibitors, Benzimidazoles chemical synthesis, Protein Kinase Inhibitors chemical synthesis
- Abstract
A new series of Schiff bases containing benzіmidazole moiety 11-17 were synthesized by the reaction of 4-(1H-benzо[d]іmіdazоl-2-yl)anіline (1) with different aromatic aldehydes (4-10) via conventional heating and microwave irradiation methods. The structures of the novel Schiff bases were characterized by using different spectral data. Also, metal complexes 18-21 of compound 13 were synthesized, and their structure was confirmed by spectral measurements (IR, NMR, UV), molar conductivity, magnetic susceptibility and thermo-gravimetric analysis. The novel synthesized ligand 13 and its complexes 18-21 were tested for their in vitro antitumor activities towards breast, liver and lung cancer cell lines. Also, the acute toxicity of the prepared compounds 13 and 18-21 was determined in vivo. The results showed that the newly synthesized compounds 13 and 18-21 exhibited a significant activity against cancer, especially for complex 21, compared to standard drug doxorubicin. The molecular docking of complexes 20 and 21 has been also studied as Aurora kinase inhibitors.
- Published
- 2018
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