Paper
Synthesis, Biological Evaluation, and Molecular Docking of New Benzimidazole-1,2,3-Triazole Hybrids as Antibacterial and Antitumor Agents
Published May 1, 2022 · Shareefa Ahmed Saleh Alzahrani, Syed Nazreen, A. Elhenawy
Polycyclic Aromatic Compounds
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Abstract
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.
New benzimidazole-1,2,3-triazole hybrids show promising antibacterial and antitumor properties, with compound 6 showing the most potent activity against MCF-7 cells.
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