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