1. Synthesis of methoxy-substituted chalcones and in vitro evaluation of their anticancer potential.
- Author
-
Ethiraj KR, Aranjani JM, and Khan FR
- Subjects
- Aldehydes chemistry, Antineoplastic Agents chemistry, Cell Cycle Checkpoints drug effects, Cell Line, Tumor, Cell Survival drug effects, Chalcones chemical synthesis, Chromatin drug effects, Chromatin metabolism, DNA Breaks, Double-Stranded drug effects, HeLa Cells, Humans, Naphthalenes chemistry, Antineoplastic Agents chemical synthesis, Antineoplastic Agents pharmacology, Chalcones chemistry, Chalcones pharmacology
- 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., (© 2013 John Wiley & Sons A/S.)
- Published
- 2013
- Full Text
- View/download PDF