Synthesis of New Enantiopure Aminoalcohol Fluorenes as Promising Antimalarial Compounds.

ABSTRACT: Herein, we report the design, synthesis, and characterisation of a new library of enantiopure aminoalcohol fluorenes, as well as their in vitro evaluation for biological properties, including activity against two strains of P. falciparum (3D7 and W2) and cytotoxicity on the HepG2 cell line. All tested compounds exhibited good to excellent antimalarial potency with IC₅₀ values ranging from 0.7 to 70.2 nM whatever the strain. Interestingly, most compounds showed equal or better antimalarial activity compared to the reference drugs lumefantrine, mefloquine and chloroquine. Despite moderate cytotoxicity in the micromolar range, all aminoalcohol fluorenes displayed an excellent selectivity index higher than 100 due to strong antimalarial activity. Furthermore, we report in silico ana

SUBMITTER: Tisnerat C 

PROVIDER: S-EPMC11911300 | biostudies-literature | 2025 Mar

REPOSITORIES: biostudies-literature