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Molecules 2012, 17(10), 11456-11468; doi:10.3390/molecules171011456

Synthesis and Anticancer Activity of Di(3-thienyl)methanol and Di(3-thienyl)methane

1, 2, 2, 2, 1, 1 and 2,*
1 Plasma Bioscience Research Center, Kwangwoon University, Seoul 139-701, Korea 2 Department of Chemistry, Kwangwoon University, Seoul 139-701, Korea
* Author to whom correspondence should be addressed.
Received: 2 August 2012 / Revised: 24 September 2012 / Accepted: 25 September 2012 / Published: 27 September 2012
(This article belongs to the Section Medicinal Chemistry)
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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 µg/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.
Keywords: thienyl derivatives; T98G gliomas; HEK cells thienyl derivatives; T98G gliomas; HEK cells
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Kaushik, N.K.; Kim, H.S.; Chae, Y.J.; Lee, Y.N.; Kwon, G.-C.; Choi, E.H.; Kim, I.T. Synthesis and Anticancer Activity of Di(3-thienyl)methanol and Di(3-thienyl)methane. Molecules 2012, 17, 11456-11468.

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