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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; in revised form: 24 September 2012 / Accepted: 25 September 2012 / Published: 27 September 2012
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 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
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MDPI and ACS Style
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.
Kaushik NK, Kim HS, Chae YJ, Lee YN, Kwon G-C, Choi EH, Kim IT. Synthesis and Anticancer Activity of Di(3-thienyl)methanol and Di(3-thienyl)methane. Molecules. 2012; 17(10):11456-11468.
Kaushik, Nagendra Kumar; Kim, Hong Seon; Chae, Young June; Lee, Young Nam; Kwon, Gi-Chung; Choi, Eun Ha; Kim, In Tae. 2012. "Synthesis and Anticancer Activity of Di(3-thienyl)methanol and Di(3-thienyl)methane." Molecules 17, no. 10: 11456-11468.