0000000000277080
AUTHOR
Hanife Bahsi
The broad-spectrum antiinfective drug artesunate interferes with the canonical nuclear factor kappa B (NF-κB) pathway by targeting RelA/p65.
Infection with human cytomegalovirus (HCMV) is a serious medical problem, particularly in immunocompromised individuals and neonates. The success of standard antiviral therapy is hampered by low drug compatibility and induction of viral resistance. A novel strategy is based on the exploitation of cell-directed signaling inhibitors. The broad antiinfective drug artesunate (ART) offers additional therapeutic options such as oral bioavailability and low levels of toxic side-effects. Here, novel ART-derived compounds including dimers and trimers were synthesized showing further improvements over the parental drug. Antiviral activity and mechanistic aspects were determined leading to the followi…
New efficient artemisinin derived agents against human leukemia cells, human cytomegalovirus and Plasmodium falciparum: 2nd generation 1,2,4-trioxane-ferrocene hybrids
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 …
CCDC 994084: Experimental Crystal Structure Determination
Related Article: Christoph Reiter, Tony Fröhlich, Maen Zeino, Manfred Marschall, Hanife Bahsi, Maria Leidenberger, Oliver Friedrich, Barbara Kappes, Frank Hampel, Thomas Efferth, Svetlana B. Tsogoeva|2015|Eur.J.Med.Chem.|97|164|doi:10.1016/j.ejmech.2015.04.053
CCDC 994085: Experimental Crystal Structure Determination
Related Article: Christoph Reiter, Tony Fröhlich, Maen Zeino, Manfred Marschall, Hanife Bahsi, Maria Leidenberger, Oliver Friedrich, Barbara Kappes, Frank Hampel, Thomas Efferth, Svetlana B. Tsogoeva|2015|Eur.J.Med.Chem.|97|164|doi:10.1016/j.ejmech.2015.04.053