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Synthesis, Biological Profile, and Molecular Docking of Some New Bis- Imidazole Fused Templates and Investigation of Their Cytotoxic Potential as Anti-tubercular and/or Anticancer Prototypes


Refaie M. Kassab, Sobhi M. Gomha, Zeinab A. Muhammad* and Ahmed S. El-khouly   Pages 1 - 12 ( 12 )


Background: There is a great need to discover more drugs with antimycobacterial activities to fight lung cancer and tuberculosis (two of the deadliest diseases world-wide). To our knowledge, the present study is the first to report antimycobacterial activity of imidazole-fused heterocycles.

Objective: Construction of some bis-imidazole fused heterocycles with potential anti-tubercular and/or potent antitumor activities.

Method: A series of bis-imidazole fused derivatives 6-8 and 13-16 was constructed using bis-phenacyl bromide derivative 2 as a synthetic platform. Compound 2 was also used to access bis-quinoxaline 20, bis-benzothiazine derivatives 23, and bisthiazolopyrimidine derivatives 26. The new bis-imidazole derivatives were evaluated for their anticancer activity against lung carcinoma cell line (A-549) using Cisplatin as a reference drug. The new compounds were also screened for their antitubercular activity against M. tuberculosis (ATCC 25177) using Isoniazid as a reference drug.

Result: Among the new bis-imidazole derivatives, three examples showed remarkable antitumor activities while five other compounds showed high antimycobacterial activity.

Conclusion: A novel series of bis-imidazole fused heterocycles was developed. Multiple prototypes of this new series showed remarkable anti-tubercular and/or potent antitumor activities.


Bis-heterocycles, imidazotriazoles, imidazothiazoles, thiazolopyrimidines, anti-tumor and anti-tubercular activities.


Department of Chemistry, Faculty of Science, Cairo University, Giza 12613, Department of Chemistry, Faculty of Science, Cairo University, Giza 12613, Department of Organic Chemistry, National Organization for Drug Control and Research (NODCAR), Giza 12311, Department of Organic & Medicinal Chemistry, Faculty of Pharmacy, University of Sadat City

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