0000000000610445

AUTHOR

Manolis A. Fousteris

showing 1 related works from this author

Synthesis and cytotoxic activity of new artemisinin hybrid molecules against human leukemia cells

2017

A series of new artemisinin-derived hybrids which incorporate cholic acid moieties have been synthesized and evaluated for their antileukemic activity against sensitive CCRF-CEM and multidrug-resistant CEM/ADR5000 cells. The new hybrids 20-28 showed IC50 values in the range of 0.019µM-0.192µM against CCRF-CEM cells and between 0.345µM and 7.159µM against CEM/ADR5000 cells. Amide hybrid 25 proved the most active compound against both CCRF-CEM and CEM/ADR5000 cells with IC50 value of 0.019±0.001µM and 0.345±0.031µM, respectively. A relatively low cross resistance to hybrids 20-28 in the range of 5.7-fold to 46.1-fold was measured. CEM/ADR5000 cells showed higher resistance than CCRF-CEM to al…

0301 basic medicinevirusesClinical BiochemistryPharmaceutical ScienceAntineoplastic AgentsBiochemistryAntileukemic agentStructure-Activity Relationship03 medical and health scienceschemistry.chemical_compound0302 clinical medicineimmune system diseaseshemic and lymphatic diseasesAmideDrug DiscoveryTumor Cells CulturedmedicineHumansCytotoxic T cellDoxorubicinArtemisininMolecular BiologyIC50Cross-resistanceCell ProliferationLeukemiaDose-Response Relationship DrugMolecular StructureOrganic ChemistryCholic acidhemic and immune systemsArtemisinins030104 developmental biologyBiochemistrychemistry030220 oncology & carcinogenesisMolecular MedicineDrug Screening Assays Antitumormedicine.drugBioorganic & Medicinal Chemistry
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