title: Dibenzylideneacetone analogues as novel Plasmodium falciparum inhibitors.
abstract: A series of dibenzylideneacetones (A1-A12) and some of their pyrazolines (B1-B4) were synthesized and evaluated in vitro for blood stage antiplasmodial properties in Plasmodium falciparum culture using SYBR-green-I fluorescence assay. The compound (1E, 4E)-1,5-bis(3,4-dimethoxyphenyl)penta-1,4-dien-3-one (A9) was found to be the most active with IC(50) of 1.97 μM against chloroquine-sensitive strain (3D7) and 1.69 μM against chloroquine-resistant field isolate (RKL9). The MTT based cytotoxicity assay on HeLa cell line has confirmed that A9 is selective in its action against malaria parasite (with a therapeutic index of 166). Our results revealed that these compounds exhibited promising antiplasmodial activities which can be further explored as potential leads for the development of cheaper, safe, effective and potent drugs against chloroquine-resistant malarial parasites.
authors.affiliation: Department of Pharmacy, Shri G.S. Institute of Technology and Science, 23 Park Road, Indore 452003 (MP), India. rahulba26@yahoo.co.in
authors.forename: Rahul Balasaheb
authors.initials: RB
authors.lastname: Aher
authors.forename: Gajanan
authors.initials: G
authors.lastname: Wanare
authors.forename: Neha
authors.initials: N
authors.lastname: Kawathekar
authors.forename: Ravi Ranjan
authors.initials: RR
authors.lastname: Kumar
authors.forename: Naveen Kumar
authors.initials: NK
authors.lastname: Kaushik
authors.forename: Dinkar
authors.initials: D
authors.lastname: Sahal
authors.forename: Virander Singh
authors.initials: VS
authors.lastname: Chauhan
mesh_terms: D000096:Acetone / Q000737:chemistry* / Q000494:pharmacology; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001597:Benzylidene Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D006367:HeLa Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D010963:Plasmodium falciparum / Q000187:drug effects*; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000962:Antimalarials; D001597:Benzylidene Compounds; D011720:Pyrazoles; D000096:Acetone