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

Journal article
(Original article)


Publication Details

Author(s): Reiter C, Fröhlich T, Zeino M, Marschall M, Bahsi H, Leidenberger M, Friedrich O, Kappes B, Hampel F, Efferth T, Tsogoeva S
Journal: European journal of medicinal chemistry
Publication year: 2015
Volume: 97
Pages range: 164-72
ISSN: 1768-3254
Language: English


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.



FAU Authors / FAU Editors

Friedrich, Oliver Prof. Dr. Dr.
Lehrstuhl für Medizinische Biotechnologie
Fröhlich, Tony
Lehrstuhl für Organische Chemie I
Hampel, Frank Dr.
Lehrstuhl für Organische Chemie I
Kappes, Bärbel Prof. Dr.
Lehrstuhl für Medizinische Biotechnologie
Leidenberger, Maria
Lehrstuhl für Medizinische Biotechnologie
Reiter, Christoph
Professur für Organische Chemie
Tsogoeva, Svetlana Prof. Dr.
Professur für Organische Chemie


External institutions with authors

Johannes Gutenberg-Universität Mainz


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://dx.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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Last updated on 2019-21-07 at 07:14