title: Cyclopalladated organosilane-tethered thiosemicarbazones: novel strategies for improving antiplasmodial activity.
abstract: Two series of ferrocenyl- and aryl-derived cyclopalladated organosilane thiosemicarbazone complexes were synthesised via C-H bond activation. Selected compounds were evaluated for in vitro antiplasmodial activity against the chloroquine-sensitive (NF54) and chloroquine-resistant (Dd2) strains of the human malaria parasite Plasmodium falciparum. Cyclopalladation of the thiosemicarbazones resulted in antiplasmodial activities in the low micromolar range.
authors.affiliation: Department of Chemistry, University of Cape Town, Private Bag, Rondebosch 7701, South Africa. gregory.smith@uct.ac.za.
authors.forename: Muneebah
authors.initials: M
authors.lastname: Adams
authors.forename: Linley
authors.initials: L
authors.lastname: Barnard
authors.forename: Carmen
authors.initials: C
authors.lastname: de Kock
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Smith
authors.forename: Lubbe
authors.initials: L
authors.lastname: Wiesner
authors.forename: Kelly
authors.initials: K
authors.lastname: Chibale
authors.forename: Gregory S
authors.initials: GS
authors.lastname: Smith
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000737:chemistry* / Q000494:pharmacology / Q000633:toxicity; D016466:CHO Cells; D002470:Cell Survival / Q000187:drug effects; D002738:Chloroquine / Q000494:pharmacology / Q000633:toxicity; D006224:Cricetinae; D003412:Cricetulus; D004351:Drug Resistance / Q000187:drug effects; D010963:Plasmodium falciparum / Q000187:drug effects; D012821:Silanes / Q000737:chemistry*; D013882:Thiosemicarbazones / Q000737:chemistry*
chemical_list: D000962:Antimalarials; D012821:Silanes; D013882:Thiosemicarbazones; D002738:Chloroquine