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Molecules 2012, 17(10), 11456-11468;

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

Plasma Bioscience Research Center, Kwangwoon University, Seoul 139-701, Korea
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. View Full-Text
Keywords: thienyl derivatives; T98G gliomas; HEK cells thienyl derivatives; T98G gliomas; HEK cells

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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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