Synthesis and in vitro SAR evaluation of natural vanillin-based chalcones tethered quinolines as antiplasmodial agents

A series of novel chalcone derivatives were synthesized and investigated against the chloroquine-sensitive P. falciparum 3D7 (Pf3D7) strain chloroquine-resistant K1 to establish their structure-activity relationship. In this study, compound 7 was found most active as well less cytotoxic (IC50 = 4.12 µM 3.14 for Pf3D7 PfK1 respectively; CC50 46.18 µM). Compound studied effect on parasite growth microscopic examination showed excessive DNA damage in trophozoite stage. The recovery after drug removal poor due dramatic genotoxic 7. It suggested that 7-chloro quinoline triazole linkage crucial antimalarial potential. Graphical abstract