Synthesis and Anticancer Potential of New Benzimidazole Theranostic

Area of Science:

• Medicinal Chemistry
• Cancer Biology
• Biophysics

Background:

• Developing novel anticancer agents is crucial for treating oral squamous cell carcinoma (OSCC) and colorectal carcinoma.
• Benzimidazole derivatives have shown promise as therapeutic agents.
• Targeting sirtuin 2 (SIRT2) is a potential strategy for cancer therapy.

Purpose of the Study:

• To design, synthesize, and evaluate novel benzimidazole analogs for anticancer activity.
• To investigate the potential of these compounds as SIRT2 inhibitors.
• To explore the theranostic potential of promising candidates.

Main Methods:

• Synthesis of benzimidazole analogs.
• Screening against OSCC (H103, H314) and colorectal carcinoma (HCT116) cell lines.
• Structural characterization using NMR and LC-MS.
• SIRT2 inhibition assay and molecular docking.
• Fluorescence property analysis.

Main Results:

• Compound V7 demonstrated significant broad-spectrum anticancer activity with IC50 values in the low micromolar range.
• V7 exhibited potent SIRT2 inhibitory activity.
• Molecular docking indicated the importance of a hydroxyl group for SIRT2 inhibition.
• V7 possesses high autofluorescence, suggesting theranostic capabilities.

Conclusions:

• The synthesized benzimidazole analogs represent a promising class of anticancer agents.
• Compound V7 is a potent anticancer candidate with potential as a SIRT2 inhibitor.
• The autofluorescent properties of V7 open avenues for its development as a theranostic agent.