6533b821fe1ef96bd127b6b1

RESEARCH PRODUCT

Synthesis and biological evaluation of antimalarial and antileukemic activity of new C-10 modified artemisinin derivatives

Marcel KaiserMarcel KaiserToni SmeilusDimanthi PliatsikaFarnoush MousavizadehThomas EfferthAthanassios GiannisDaniel Meyer

subject

chemistry.chemical_classificationCell growthOrganic ChemistryPharmacologymedicine.diseaseBiochemistryAldehydechemistry.chemical_compoundLeukemiachemistryArtesunateChloroquineDrug DiscoverymedicineAzideArtemisininmedicine.drugBiological evaluation

description

Abstract Several non-acetal artemisinin derivatives were synthesized and their antimalarial activity against chloroquine-resistant parasites as well as their antileukemic activity were investigated. The azide 10 was proved to have slightly better activity than the current antimalarial drugs such as artesunate and chloroquine. In addition, the azide 10 and the aldehyde 7 were found to be effective in decreasing cell proliferation in leukemia cells.

https://doi.org/10.1016/j.tet.2021.132410