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Synthesis of Tetrahydrohonokiol Derivates and Their Evaluation for Cytotoxic Activity against CCRF-CEM Leukemia, U251 Glioblastoma and HCT-116 Colon Cancer Cells

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Department of Pharmaceutical Chemistry, Institute of Pharmaceutical Sciences, Universitätsplatz 1, University of Graz, 8010 Graz, Austria
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Department of Pharmacognosy, Institute of Pharmaceutical Sciences, Universitätsplatz 4, University of Graz, 8010 Graz, Austria
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Institute of Zoologie, Universitätsplatz 2, University of Graz, 8010 Graz, Austria
*
Author to whom correspondence should be addressed.
Molecules 2014, 19(1), 1223-1237; https://doi.org/10.3390/molecules19011223
Received: 9 December 2013 / Revised: 9 January 2014 / Accepted: 13 January 2014 / Published: 20 January 2014
(This article belongs to the Section Medicinal Chemistry)
Biphenyl neolignans such as honokiol and magnolol, which are the major active constituents of the Asian medicinal plant Magnolia officinalis, are known to exert a multitude of pharmacological and biological activities. Among these, cytotoxic and tumor growth inhibitory activity against various tumour cell lines are well-documented. To further elucidate the cytotoxic effects of honokiol derivatives, derivatizations were performed using tetrahydrohonokiol as a scaffold. The derivatizations comprised the introduction of functional groups, e.g., nitro and amino groups, as well as alkylation. This way, 18 derivatives, of which 13 were previously undescribed compounds, were evaluated against CCRF-CEM leukemia cells, U251 glioblastoma and HCT-116 colon cancer cells. The results revealed no significant cytotoxic effects in any of the three tested cell lines at a test concentration of 10 µM. View Full-Text
Keywords: tetrahydrohonokiol derivatives; cytotoxicity; CCRF-CEM leukemia cells; U251 glioblastoma; HCT-116 colon cancer cells; Magnolia officinalis tetrahydrohonokiol derivatives; cytotoxicity; CCRF-CEM leukemia cells; U251 glioblastoma; HCT-116 colon cancer cells; Magnolia officinalis
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Bernaskova, M.; Kretschmer, N.; Schuehly, W.; Huefner, A.; Weis, R.; Bauer, R. Synthesis of Tetrahydrohonokiol Derivates and Their Evaluation for Cytotoxic Activity against CCRF-CEM Leukemia, U251 Glioblastoma and HCT-116 Colon Cancer Cells. Molecules 2014, 19, 1223-1237.

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