MALAYSIAN JOURNAL OF CHEMISTRY (MJChem)

MJChem is double-blind peer reviewed journal published by the Malaysian Institute of Chemistry (Institut Kimia Malaysia) E-ISSN: 2550-1658

Synthesis of Benzhydrol-type Derivatives as Stable 1′-Acetoxychavicol Acetate Analogues, Cytotoxic Evaluation and Molecular Docking Study

Mohamad Nurul Azmi
Universiti Sains Malaysia
Kok Hoong Leong
University of Malaya
Muhammad Solehin Abd Ghani
Universiti Sains Malaysia
Nur Farah Atiqah Azmi
Universiti Sains Malaysia
Mohammad Tasyriq Che Omar
Universiti Sains Malaysia
Khalijah Awang
University of Malaya

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.

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Published 24 February 2025


Issue Vol 27 No 1 (2025): Malaysian Journal of Chemistry

Section