title: Antimalarial activity of newly synthesized chalcone derivatives in vitro.
abstract: Twenty-seven novel chalcone derivatives were synthesized using Claisen-Schmidt condensation and their antimalarial activity against asexual blood stages of Plasmodium falciparum was determined. Antiplasmodial IC(50)  (half-maximal inhibitory concentration) activity of a compound against malaria parasites in vitro provides a good first screen for identifying the antimalarial potential of the compound. The most active compound was 1-(4-benzimidazol-1-yl-phenyl)-3-(2, 4-dimethoxy-phenyl)-propen-1-one with IC(50)  of 1.1 μg/mL, while that of the natural phytochemical, licochalcone A is 1.43 μg/mL. The presence of methoxy groups at position 2 and 4 in chalcone derivatives appeared to be favorable for antimalarial activity as compared to other methoxy-substituted chalcones. Furthermore, 3, 4, 5-trimethoxy groups on chalcone derivative probably cause steric hindrance in binding to the active site of cysteine protease enzyme, explaining the relative lower inhibitory activity.
authors.affiliation: Department of Chemistry, University of Delhi, Delhi 110007, India             Department of Zoology, University of Delhi, Delhi 110007, India.
authors.forename: Neesha
authors.initials: N
authors.lastname: Yadav
authors.forename: Sandeep K
authors.initials: SK
authors.lastname: Dixit
authors.forename: Amit
authors.initials: A
authors.lastname: Bhattacharya
authors.forename: Lokesh C
authors.initials: LC
authors.lastname: Mishra
authors.forename: Manish
authors.initials: M
authors.lastname: Sharma
authors.forename: Satish K
authors.initials: SK
authors.lastname: Awasthi
authors.forename: Virendra K
authors.initials: VK
authors.lastname: Bhasin
mesh_terms: D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002599:Chalcone / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D004912:Erythrocytes / Q000469:parasitology; D006801:Humans; D020128:Inhibitory Concentration 50; D016778:Malaria, Falciparum / Q000188:drug therapy; D010963:Plasmodium falciparum / Q000187:drug effects*
chemical_list: D000962:Antimalarials; D002599:Chalcone