Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 97, Issue -, Pages 164-172Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2015.04.053
Keywords
Artemisinin; Ferrocene; Hybrid; Cancer; Malaria; Human cytomegalovirus
Categories
Funding
- Deutsche Forschungsgemeinschaft (DFG)
- Wilhelm Sander-Stiftung
- Interdisciplinary Center for Molecular Materials (ICMM)
- Wilhelm Sander-Stiftung [2011.085.1, 2011.085.2]
- Deutsche Forschungsgemeinschaft [MA 1289/7-1]
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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 mu M). 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 mu M). 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 mu M) against human cytomegalovirus (HCMV). The application of 1,2,4-trioxane-ferrocene hybrids against HCMV is unprecedented and demonstrated here for the first time. (C) 2015 Elsevier Masson SAS. All rights reserved.
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