Synthesis and anticancer activity of di(3-thienyl)methanol and di(3-thienyl)methane

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Abstract

Di(3-thienyl)methanol (2) and di(3-thienyl)methane (3) have been synthesized and screened against the T98G (brain cancer) cell line. Treatment induced cell death (MTT and macro-colony assay), growth inhibition, cytogenetic damage (micronuclei formation), were studied as cellular response parameters. Treatment with the compounds enhanced growth inhibition and cell death in a concentration dependent manner in both T98G and HEK (normal) cell lines. At higher concentrations (>20 μ g/mL) the cytotoxic effects of the compounds were highly significant. The effect on clonogenic capacity and micronuclei formation observed after treatment of cells. Amongst the compounds, compound 2 exhibited potent activity against T98G brain cancer cells. Despite potent in vitro activity, both compounds exhibited less cytotoxicity against normal human HEK cells at all effective concentrations. © 2012 by the authors; licensee MDPI, Basel, Switzerland.

Figures

  • Figure 1. Energy minimized 3D structure of di(3-thienyl)methanol (2) and di(3-thienyl)methane (3). Red, yellow, white color ball represents oxygen, sulfur and hydrogen atoms respectively. Pink balls represent lone pairs on the oxygen atom.
  • Figure 2. % Viability evaluated from MTT assay on T98G brain cancer and normal HEK cells treated with thienyl derivative for 24, 48, and 72 h.
  • Figure 4. Morphology of compound 2 treated T98G brain cancer cells at 24 h after treatment. Cells were treated at concentration 2.2, 6.6, 20, 60 and 200 µg/mL.
  • Figure 5. Effect of compound 2 on colony forming capacity and survival of exponentially growing T98G cell lines studied by macro colony assay. Data presented are mean values from three independent observations, n = 3.
  • Figure 6. Comparison between micronucleus (MN) frequencies at 24 and 48 h in human T98G cells treated with compound 2. Whereas ‘Control’ is micronuclei frequency of untreated cells.Results are measured in vitro both in mononucleated cells and binucleated cells in cultures. These cells shown with one or many micronucleus were scored for MN frequency. The data represents mean ± SEM, n = 3.
  • Figure 7. In silico drug safety analysis for thienyl derivatives by Osiris software.
  • Table 1. Pharmacokinetic parameters (Catalyst, Chemaxon and Osiris softwares).

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CITATION STYLE

APA

Kaushik, N. K., Kim, H. S., Chae, Y. J., Lee, Y. N., Kwon, G. C., Choi, E. H., & Kim, I. T. (2012). Synthesis and anticancer activity of di(3-thienyl)methanol and di(3-thienyl)methane. Molecules, 17(10), 11456–11468. https://doi.org/10.3390/molecules171011456

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