Synthesis of Benzhydrol-type Derivatives as Stable 1′-Acetoxychavicol Acetate Analogues, Cytotoxic Evaluation and Molecular Docking Study
DOI: https://doi.org/10.55373/mjchem.v27i1.92
Keywords: Benzhydrol-type analogues; 1′-Acetoxychavicol acetate (ACA); Cytotoxic; MTT assay; Molecular Docking; IκBα protein
Abstract
Four benzhydrol analogues were synthesised, characterised and evaluated for their cytotoxic activity against two human lung carcinoma cell lines (H1975 and A549), and one colorectal carcinoma cell line (HCT116). Compound 3b (IC50 = 5.9 µM) and 3c (IC50 = 9.9 µM) show a good cytotoxic potency on H1975 cell line compared with gefitinib as a positive control (IC50 = 56.2 µM). Molecular docking was done to understand the interactions between ligand and the Nuclear Factor-KappaB Kinase alpha (IκBα) protein. These findings suggest that the benzhydrol analogues, particularly 3b and 3c, show a promising potential as anticancer agents.