Fast-Acting Chalcogen-Phosphoranes Inhibit Sensitive and Resistant <i>Plasmodium falciparum</i> Strains.

ABSTRACT: Malaria remains a major global health challenge with growing resistance to current antimalarial drugs. In this study, we report the antiplasmodial activity of eight sulfur-containing chalcogen-phosphorane analogues that show submicromolar potency against Plasmodium falciparum 3D7 strain (IC₅₀s = 0.7-1.9 μM) and reasonable selectivity indexes (SI) over HepG2 and HEK293 cells (SI ≥ 12). Electron-withdrawing substituents on the aromatic ring improved potency by two- to 3-fold. Compound 5, a representative compound of the series, showed fast-acting inhibitory activity that rapidly induced pyknotic nuclei, demonstrated no cross-resistance with standard antimalarials, and exhibited an additive interaction with artesunate. Stage-specific assays revealed pronounced activit

SUBMITTER: Moura IMR 

PROVIDER: S-EPMC12824749 | biostudies-literature | 2026 Jan

REPOSITORIES: biostudies-literature