title: Synthesis and in vitro antimalarial activity of tetraoxane-amine/amide conjugates.
abstract: A series of tetraoxanes, tetraoxane-amine and tetraoxane-amide conjugates have been synthesized and screened for in vitro antimalarial activity against chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum. Most of the conjugates showed slightly better antimalarial activity than the parent tetraoxanes. Three of the conjugate compounds were potentially active with IC(50) values in the range of 0.38-0.80μM. Cytotoxicity of four selected compounds was also evaluated in a panel of four cancer (SK-MEL, KB, BT-549, SK-OV-3) and two non-cancer (Vero and LLC-PK(11)) cell lines up to a concentration of 25μM and none of the compounds was found toxic to any of the cells.
authors.affiliation: Department of Chemistry, University of Delhi, Delhi 110007, India.
authors.forename: Nitin
authors.initials: N
authors.lastname: Kumar
authors.forename: Shabana I
authors.initials: SI
authors.lastname: Khan
authors.forename: Himanshu
authors.initials: H
authors.lastname: Atheaya
authors.forename: Ritu
authors.initials: R
authors.lastname: Mamgain
authors.forename: Diwan S
authors.initials: DS
authors.lastname: Rawat
mesh_terms: D000577:Amides / Q000737:chemistry; D000588:Amines / Q000737:chemistry; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology; D037621:Artemisinins / Q000494:pharmacology; D045744:Cell Line, Tumor; D002522:Chlorocebus aethiops; D002738:Chloroquine / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004351:Drug Resistance; D006801:Humans; D020128:Inhibitory Concentration 50; D010963:Plasmodium falciparum / Q000187:drug effects*; D013329:Structure-Activity Relationship; D045568:Tetraoxanes / Q000138:chemical synthesis* / Q000494:pharmacology; D014709:Vero Cells
chemical_list: D000577:Amides; D000588:Amines; D000962:Antimalarials; D037621:Artemisinins; D045568:Tetraoxanes; D002738:Chloroquine; C031327:artemisinin