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Synthesis of Methoxy-substituted Chalcones and in vitro Evaluation of their Anticancer Potential

Authors

  • Kannatt Radhakrishnan Ethiraj,

    1. Pharmaceutical Chemistry Division, School of Advance Sciences, VIT University, Vellore, Tamil Nadu, India
    2. Organic and Medicinal Chemistry Research Laboratory, School of Advance Sciences, VIT University, Vellore, Tamil Nadu, India
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  • Jesil Mathew Aranjani,

    1. Department of Pharmaceutical Biotechnology, Manipal College of Pharmaceutical Sciences, Manipal University, Udupi, Karnataka, India
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  • Fazlur-Rahman Nawaz Khan

    Corresponding author
    1. Organic and Medicinal Chemistry Research Laboratory, School of Advance Sciences, VIT University, Vellore, Tamil Nadu, India
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Abstract

Methoxy-substituted chalcones, 3 were obtained using simple, efficient method from 2-naphtylethanone, 1 and aromatic aldehydes, 2. The in vitro cytotoxicity activities of the chalcones against a panel of three human cancer cell lines were explored. The tested compounds were found to possess significant cytotoxic activity. The DNA strand break and damage was quantified through alkaline comet assay, flow cytometric analysis, and chromatin condensation studies, which revealed the apoptotic nature of the compounds. Compound 3c, (3-(3,4,5-trimethoxyphenyl)-1-(2-naphthyl) prop-2-en-1-one) showed highest cytotoxicity of 0.019 μm against HeLa, 0.020 μm against HCT15 and 0.022 μm against A549. Compound 3e, (3-(3,5-dimethoxyphenyl)-1-(2-naphthyl) prop-2-en-1-one) showed better IC50 values against all the three cell lines employed for the study.

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