New efficient artemisinin derived agents against human leukemia cells, human cytomegalovirus and Plasmodium falciparum: 2nd generation 1,2,4-trioxane-ferrocene hybrids.

Reiter C, Fröhlich T, Zeino M, Marschall M, Bahsi H, Leidenberger M, Friedrich O, Kappes B, Hampel F, Efferth T, Tsogoeva S (2015)

Publication Language: English

Publication Status: Published

Publication Type: Journal article, Original article

Publication year: 2015

Journal

European Journal of Medicinal Chemistry Elsevier

Book Volume: 97

Pages Range: 164-72

URI: http://www.sciencedirect.com/science/article/pii/S0223523415300179

DOI: 10.1016/j.ejmech.2015.04.053

Abstract

In our ongoing search for highly active hybrid molecules exceeding their parent compounds in anticancer, antimalaria as well as antiviral activity and being an alternative to the standard drugs, we present the synthesis and biological investigations of 2nd generation 1,2,4-trioxane-ferrocene hybrids. In vitro tests against the CCRF-CEM leukemia cell line revealed di-1,2,4-trioxane-ferrocene hybrid 7 as the most active compound (IC50 of 0.01 μM). Regarding the activity against the multidrug resistant subline CEM/ADR5000, 1,2,4-trioxane-ferrocene hybrid 5 showed a remarkable activity (IC50 of 0.53 μM). Contrary to the antimalaria activity of hybrids 4-8 against Plasmodium falciparum 3D7 strain with slightly higher IC50 values (between 7.2 and 30.2 nM) than that of their parent compound DHA, hybrids 5-7 possessed very promising activity (IC50 values lower than 0.5 μM) against human cytomegalovirus (HCMV). The application of 1,2,4-trioxane-ferrocene hybrids against HCMV is unprecedented and demonstrated here for the first time.

Authors with CRIS profile

Christoph Reiter Professur für Organische Chemie Tony Fröhlich Lehrstuhl für Organische Chemie I Manfred Marschall Lehrstuhl für Klinische und Molekulare Virologie Maria Leidenberger Lehrstuhl für Medizinische Biotechnologie Oliver Friedrich Lehrstuhl für Medizinische Biotechnologie Bärbel Kappes Lehrstuhl für Medizinische Biotechnologie Frank Hampel Lehrstuhl für Organische Chemie I Svetlana Tsogoeva Professur für Organische Chemie

Involved external institutions

Johannes Gutenberg-Universität Mainz (JGU) DE Germany (DE)

How to cite

APA:

Reiter, C., Fröhlich, T., Zeino, M., Marschall, M., Bahsi, H., Leidenberger, M.,... Tsogoeva, S. (2015). New efficient artemisinin derived agents against human leukemia cells, human cytomegalovirus and Plasmodium falciparum: 2nd generation 1,2,4-trioxane-ferrocene hybrids. European Journal of Medicinal Chemistry, 97, 164-72. https://doi.org/10.1016/j.ejmech.2015.04.053

MLA:

Reiter, Christoph, et al. "New efficient artemisinin derived agents against human leukemia cells, human cytomegalovirus and Plasmodium falciparum: 2nd generation 1,2,4-trioxane-ferrocene hybrids." European Journal of Medicinal Chemistry 97 (2015): 164-72.

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