Search results for "4-Trioxane"

showing 2 items of 2 documents

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

2015

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 …

Human cytomegalovirusMetallocenesPlasmodium falciparumHeterocyclic Compounds 4 or More RingsInhibitory Concentration 50chemistry.chemical_compoundHeterocyclic CompoundsCell Line TumorDrug DiscoverymedicineHumansFerrous CompoundsArtemisininIC50HybridPharmacologyLeukemiabiologyOrganic ChemistryPlasmodium falciparumGeneral Medicinebiology.organism_classificationmedicine.diseaseVirologyArtemisininsDrug Resistance MultipleMultiple drug resistanceBiochemistryFerrocenechemistry124-Trioxanemedicine.drugEuropean Journal of Medicinal Chemistry
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Synthesis and study of cytotoxic activity of 1,2,4-trioxane- and egonol-derived hybrid molecules against Plasmodium falciparum and multidrug-resistan…

2014

Abstract Malaria and cancer cause the death of millions of people every year. To combat these two diseases, it is important that new pharmaceutically active compounds have the ability to overcome multidrug resistance in cancer and Plasmodium falciparum strains. In search of effective anti-cancer and anti-malaria hybrids that possess improved properties compared to their parent compounds, a series of novel 1,2,4-trioxane-based hybrids incorporating egonol and/or ferrocene fragments were synthesized and tested in vitro against P. falciparum strains, CCRF–CEM cells and the multidrug-resistant P-glycoprotein-over-expressing CEM/ADR5000 cells. The most active compounds against P. falciparum stra…

StereochemistryMetallocenesPlasmodium falciparumAntineoplastic Agentschemistry.chemical_compoundAntimalarialsHeterocyclic CompoundsDrug DiscoverymedicineCytotoxic T cellHumansCell LineageFerrous CompoundsArtemisininMalaria FalciparumCytotoxicityIC50BenzofuransPharmacologyLeukemiabiologyOrganic ChemistryPlasmodium falciparumGeneral Medicinemedicine.diseasebiology.organism_classificationDrug Resistance MultipleMultiple drug resistanceLeukemiachemistryBiochemistry124-TrioxaneDrug Resistance Neoplasmmedicine.drugEuropean journal of medicinal chemistry
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