J. N. Masagalli, K. Mahadevan, H. Jayadevappa
Nov 21, 2013
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Medicinal Chemistry Research
Abstract
A series of 3-(1H-indol-3-yl)-1,3-diphenylpropan-1-ones 3a–l were synthesized in good to excellent yield by Michael addition of indole 1 with α,β-unsaturated ketones 2a–l in presence of indium(III) sulphate (20 mol%). The structure of the title compounds were established by 1H NMR, 13C NMR, mass and elemental analysis. All the synthesized compounds were evaluated for in vitro cytotoxicity against five different cancer cell lines such as ACHN (human kidney adenocarcinoma), Panc1 (pancreatic), Calu1 (lung), H460 (non small cell lung), HCT116 (human colon cancer cell) and MCF10A (normal breast epithelium) using propidium iodide staining assay protocol. The result showed that the compounds 3e and 3l have excellent cytotoxic activity with the IC50 value ranging from 1.4–2.7 to 2.4–3.4 μM, respectively, in comparison with the other compounds, Flavopiridol and Gemcitabine were employed as a positive control. The findings conferred 3-(1H-indol-3-yl)-1,3-diphenylpropan-1-ones seem to be promising candidates for the development of new anticancer drugs.