Literature DB >> 30205654

Benzimidazole - Schiff bases and their complexes: synthesis, anticancer activity and molecular modeling as Aurora kinase inhibitor.

Asmaa A Magd-El-Din1, Hanan A Mousa2, Ammar A Labib2, Ashraf S Hassan3, Amira S Abd El-All4, Mamdouh M Ali5, Ahmed A El-Rashedy4, Ahmed H El-Desoky6.   

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.

Entities:  

Keywords:  Schiff bases; benzimidazole; conventional heating; cytotoxicity; metal complexes; microwave irradiation; molecular docking

Mesh:

Substances:

Year:  2018        PMID: 30205654     DOI: 10.1515/znc-2018-0010

Source DB:  PubMed          Journal:  Z Naturforsch C J Biosci        ISSN: 0341-0382


  3 in total

1.  Design, Synthesis, Anticancer Evaluation, Enzymatic Assays, and a Molecular Modeling Study of Novel Pyrazole-Indole Hybrids.

Authors:  Ashraf S Hassan; Gaber O Moustafa; Hanem M Awad; Eman S Nossier; Mohamed F Mady
Journal:  ACS Omega       Date:  2021-04-29

2.  Discovery of New Schiff Bases Tethered Pyrazole Moiety: Design, Synthesis, Biological Evaluation, and Molecular Docking Study as Dual Targeting DHFR/DNA Gyrase Inhibitors with Immunomodulatory Activity.

Authors:  Ashraf S Hassan; Ahmed A Askar; Ahmed M Naglah; Abdulrahman A Almehizia; Ahmed Ragab
Journal:  Molecules       Date:  2020-06-02       Impact factor: 4.411

3.  Biological Evaluation and Molecular Docking with In Silico Physicochemical, Pharmacokinetic and Toxicity Prediction of Pyrazolo[1,5-a]pyrimidines.

Authors:  Ahmed M Naglah; Ahmed A Askar; Ashraf S Hassan; Tamer K Khatab; Mohamed A Al-Omar; Mashooq A Bhat
Journal:  Molecules       Date:  2020-03-21       Impact factor: 4.411

  3 in total

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