6533b7d9fe1ef96bd126c1ce
RESEARCH PRODUCT
New artesunic acid homodimers: Potent reversal agents of multidrug resistance in leukemia cells
Astrid HerrmannAysun ÇApcıSvetlana B. TsogoevaThomas EfferthChristoph Reitersubject
Cell SurvivalClinical BiochemistryPharmaceutical ScienceAntineoplastic AgentsBiochemistryStructure-Activity RelationshipDrug DiscoveryTumor Cells CulturedmedicineHumansCytotoxic T cellMolecular BiologyArtesunic acidLeukemiaDose-Response Relationship DrugMolecular StructureChemistryOrganic ChemistrySuccinatesmedicine.diseaseArtemisininsDrug Resistance MultipleMultiple drug resistanceLeukemiaBiochemistryDrug Resistance NeoplasmApoptosisMolecular MedicineDrug Screening Assays AntitumorDimerizationLinkerdescription
Abstract To evade the problem of multidrug resistance, hybridization of natural products in dimers is considered as an effective method. After the successful synthesis of three artesunic acid homodimers connected by different types of chemical linkers, we analyzed their activity against human CCRF-CEM and multidrug-resistant p -glycoprotein-overexpressing CEM/ADR 5000 leukemia cells and observed, that multidrug resistant cells were not cross-resistant to the new compounds. Collateral sensitivity was observed for artesunic acid homodimer 2. The obtained results deliver valuable information about the linker’s structure which is required for homodimers to be highly cytotoxic.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2012-09-01 | Bioorganic & Medicinal Chemistry |