Synthesis, Biological Evaluation, and Molecular Docking of New Benzimidazole-1,2,3-Triazole Hybrids as Antibacterial and Antitumor Agents
Shareefa Ahmed Saleh Alzahrania, Syed Nazreena, Ahmed A. Elhenawya b, Thikryat Neamatallahc, Mohammad Mahbooba✉
- aDepartment of Chemistry, Faculty of Science, Al Baha University, Al Baha, Kingdom of Saudi Arabia
- bChemistry Department, Faculty of Science, Al-Azhar University, Cairo, Egypt
- cDepartment of Pharmacology and Toxicology, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Kingdom of Saudi Arabia
- ✉Corresponding author
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Abstract
A new series of benzimidazole-1,2,3-triazole hybrids have been successfully accomplished by the Click chemistry of different aromatic azides and propargylated benzimidazole (4). The structural confirmations of the molecules were done by NMR, mass spectrometry, IR, and other techniques. All the newly synthesized compounds were tested for their antibacterial potentialities against two Gram-positive and two Gram-negative bacterial strains. The antibacterial results displayed comparable activity of two compounds (7) and (9) with the standard drug against S. aureus and S. epidermidis. The anticancer results showed that compounds (6, 7, 10, and 14) were more promising than tamoxifen toward MCF-7 cells. Whereas, compound (6) was the most potent molecule with IC50 3.23, 6.56, and 5.35 μM toward MCF-7, HepG2, and HCT-116 cell lines, respectively. The molecular docking showed that the synthesized molecules 6, 7, 10, and 14 with promising cytotoxicity displayed similar interaction like erlotinib with EGFR protein. These results suggest that these benzimidazole derivatives are promising lead molecules for chemotherapeutics and microbial infections.
TL;DRThe molecular docking showed that the synthesized molecules 6, 7, 10, and 14 with promising cytotoxicity displayed similar interaction like erlotinib with EGFR protein, suggesting that these benzimidazole derivatives are promising lead molecules for chemotherapeutics and microbial infections. (Semantic Scholar)